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Pharmacolgy Exam 1
pharm
125
Pharmacology
Graduate
09/16/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Drug:Botulinum Toxin Type A 
Definition

 


Mech of Action: Botox binds with the VAMPS (vesicle associated membrane proteins) and degrades them so vesicles cannot leave the presynaptic membrane. anticholinergic


Clinical Applications:. Opthalamological conditions from occular spasms: strabismus and blepharospasm; muscle dystonias and palsy; cosmetic erasure of lines wrinkles.

 

Serious and Common Adverse Events:Death from respiratory depression is systemic administration

 

Contraindications:idiopathic hypertrophy


Therapeutic Considerations: subaortic stenosis the sympathomimetic inotrope of choice for patients with acute cardiogenic circulatory failure.

Term
Drug: Botulinum toxin type B
Definition

 

Mechanism of action: pretty much the same as botulinum

Clinical applications: not approved for cosmetic uses

Term
Drug: Methyldopa
Definition

 

Mech of action: Inhibits (outcompetes) aromatic L-amino acid decarboxylase- gets converted to alpha-methyl-NE which acts as an alph2 agonist in brainstem (presynaptically) to attenuates NE release peripherally (stops release of NE in the peripheral nervous system)

 

Clinical applications: hypertension

Term
Drug: Darifenacin
Definition

 

 

Mech:Muscarinic receptor antagonists that relatively selective for glandular and smooth muscle M3 relative to M2 muscarinic receptors; shows selectivity for M3 receptors; potential utility- blocking cholinergiv bradycardia (m2) and blocking smooth muscle activity or epithelial secretions (m3)

 

Clinical applications: indicated for hyperreflexic and overactive bladder urge incontinence

 

Serious and common adverse effects: Constipation, diarrhea, nausea, dry mouth, application-site erythema, pruritus

Term
Drug: phenylnephrine
Definition

 

 

Mech of action: Selectively activate postsynaptic alpha1 adrenergic receptors; selective 1 adrenomimetic agonists

 

Clinical applications: Common cold decongestive

Term
Drug: clonidine
Definition

 


Mech:Alpha 2 agonist (mimics NE in CNS); reduces sympathetic output from CNS and is an andrenomimetic (periphery)

 

Clinical applications: anti-hypertensive


Common and serious adverse effects: hypotension, constipation, xerostomia, sedation, dizziness


Therapeutic considerations: clonidine is more potent at alpha 2 than alpha 1

Term
Drug: dobutamine
Definition

 

mech of action: beta1 agonist (selective) and also activates alpha 1 receptors; cardiac stimulant (on beta 1 receptors) promotes cardiac growth

 

Clinical applications: bradycardia, asthma attacks; hypo/hypertension, palpitations/tachcardia

Term
Drug:terbutaline (FIX)
Definition

 

mech: mimicry of transmitter at postjunctional site at beta 2. The effect is selective beta 2 receptor agonist (selective inhibition of smooth muscle contraction).

 

 Clinical applications: Terbutaline is used to delay labor in order to develop baby's lungs

Term
Drug: Metroprolol. (FIX)
Definition

 


Mech of Action: beta 1 receptor antagonist.

antagonize cardiac actions of catecholamines. Selective beta 1 blockade (cardiac)

 

Clinical Applications: slowing heart rate to improve blood flow and decrease blood pressure. decrease contactility. (?)

 

Therapeutic considerations: Causes somewhat less antagonism @ the bronchioles

Term
Drug: atenolol (FIX)
Definition

 

 

Mech: A competitive BETA-1 receptor ANTAGONIST. Blocks CARDIAC post synaptic receptors of the adrenergic system.

 

Clinical Applications: may be used for  Htn

 

Therapeutic considerations: Causes less antagonism than the bronchioles. Given to those who had a heart attack to increase survival. 

Term
Drug: imipramine
Definition

 

 

Mech:Imipramine selectively blocks NET (NE Transporter) at adrenergic synapses in the CNS. It causes a blockade of the transport system at the nerve terminal membrane. Effect of action: Accumulation of NE at receptors


Clinical application: Imipramine is a tricyclic antidepressant (TCA)- used to treat depression

Term
Drug:entacapone
Definition

 

 

Mech of action: peripherally acting Nitro catechol-type COMT inhibitor. Works by inhibition of enzymatic breakdown of transmitter in the adrenergic system. Effect- COMT inhibition attenuates/reduces levodopa toxicity on dopamine neurons- enhances dopamine action in pnts with parkinsons disease.

 

Clinical applications: entacapone (COMT inhibitor) is efficacious in the therapy of Parkingson's disease

Term
Drug: reserpine
Definition

 

 

Mech: inhibits monoamine transport into storage vesicles; leads to depletion of catecholamines of sympathetic nerve endings and brain; of serotonin, dopamine, and possibly other amines.

 

Clinical application: treat hypertension and psychotic disorder seriousL atrial fibrilation, cardiac dysrhythmia, and GI hemorrhage.

 

Common SE: GI (abdominal pain, diarrhea, nausea, vomiting, xerostomia), neurologic (dizziness, headache, lethargy, somnolence, vertigo) psychiatric (depression) respiratory (nasal congestion)

 

Contraindications: Active GI disease, depression (current or past), electroshock therapy, hypersensitivity to reserpine alkaloids, severe renal failure, ulcerative colitis.

Term
Drug: Propranolol (FIX) 
Definition

 

 

Mech: nonselective beta-blocker that reduces chronotropic, iontropic and vasodilator response to beta-adrenergic stimulation by competing for available binding sights that stimulate beta-adrendergic receptors

 

clinical application: angina pectoris, cardiac dysrhythmia, essential tremor, hypertension serious and common adverse effects: serious- cardiovascular (congestive heart failure, heart block) Dermatologic (erythema multiform, steven-johnson syndrome, toxic epidermal necrolysis). Immunologic (anaphylaxis), Respiratory (asthma bronchospasm) withdrawal symptoms. Common- dermatitis, pruritus, urticaria, dizziness, fatigue. contraindication: bronchial asthma, cardiogenic shock, if no pacemaker is present (heart block, sick sinus syndrome, sinus bradycardia)

 

Therapeutic consideration: abrupt discontinuance of propanolol causes angina and mycardial infarction.

Term
Drug: Phenoxybenzamine
Definition

 

 

mech: nonselective alpha adrenergic blockage of postganglionic synapses that is irreversible- specific for alpha 1 and alpha 2 receptors

Term
Drug: Selegiline
Definition

 

 

Mech of action: adrenergic system-irreversible selective MAO-B inhibitor-inhibition of enzymatic breakdown of transmitter

 

clinical applications: adjunct in parkingson's disease

 

therapeutic consideration: less likely to cause a marked increase in blood pressure

Term
Drug: Phenelzine
Definition

 

 

Mech of action: non-selective MAO inhibitor. irreversible antagonist of MAO

 

Clinical applications: depression, post traumatic stress

 

serious and common adverse effects: hypertensive crisis, drowsiness, weakness, dizziness dry mouth, constipation, weight gain, decreased sexual ability, uncontrollable shaking of any part of the body, muscle twitching or jerking. Serious: headache, slow, fast, or pounding heartbeat, neck stiffness or soreness, chest pain, nausea and vomiting.

 

contraindication: HTN

Term
Drug: Isocarboxazid
Definition

 

 

Mech of action: irreversible non-selective antagonist of MAO

 

Clinical application: depression

 

Serious and common adverse effects: hypertensive crisis, intercranial hemorrhage, hypotension, orthostatic seizures, hypermetabolic syndrome, serotonin syndrome, hypomania/mania hallucinations. psychosis exacerbation, toxic delirium drepression, worsening suicidaility.

 

contraindication: HTN

Term
Drug: Bethanechol
Definition

 

 

Mech: muscarinic receptor agonist has some selectivity on GI tract and urinary bladder motility

 

Clinic applications:treatment of urinary retention and inadequate emptying of the bladder, stimulates peristasis, increases motility, increases resting LES pressure.

 

Common or serious side effects: sweating, shivering, nausea, dizziness, increased frequency of urination, rhinitis (oral formulations) (AKA SLUD) 

 

contraindications: acute iritis or glaucoma after cataract extraction; narrow-angle (angle-closure) glaucoma.

 

Therapeutic consideration: almost completely selective for muscarinic receptors.

Term
Drug: pilocarpine
Definition

 

 

mech of action: muscarinic agonist; parasympathomimetic that directly stimulates cholinergic receptors.

 

Clinical application: sialagogue (enhances salivary secretion) and miotic agent (treatment of glaucoma) enhances ease of swallowing; improved oral cavity hydration

 

 Common or serious side effects- sweating is the most common; shivering, nausea, dizziness, increased frequency of urination, rhinitis (oral formulation)

 

contraindication: acute iritis or glaucoma after cataract extraction; narrow-angle (angle closure) glaucoma.

 

Therapeutic consideration: use to treat xerostomia in sjorgren's syndrome; clearance is decreased in patients with hepatic impairment, may need to reduce dose in treatment of glacoma; sufficient concentration can partially or fully reverse the ocular effects of atropine- anomalous cardiovascular responses and sweat glands are sensitive to the drug

Term
Drug:Cevimeline
Definition

 

 

Mech of Action:Muscarinic agonist; parasympathomimetic that directly stimulates cholinergic receptors

 

Clinical Applications:Sialagogue (enhances salivary secretion) and miotic agent (treatment of glaucoma); enhances ease of swallowing; improved oral cavity hydration

 

Serious and Common Adverse Events:Cholinergic side effects -- sweating is the most common; shivering, nausea, dizziness, increased frequency of urination, rhinitis (oral formulations)

 

Contraindications: Acute iritis or glaucoma after cataract extraction; Narrow-angle (angle-closure) glaucoma

 

Therapeutic Considerations:used to treat xerostomia in Sjogren's syndrome

Term
Drug:Scopolamine
Definition

 

 

Mech of Action:muscarinic receptor antagonist (antimuscarinics)

 

 Clinical Applications:Motion Sickness; Nausea & Vomiting

 

Serious and Common Adverse Events:Alteration in heart rate, drug induced psychosis, dry mouth, drowsiness, blurred vision, mydriasis (dilation of pupil) & cycloplegia (paralysis of the ciliary muscle of the eye)

 

 Contraindications:Narrow-angle glaucoma (Mydriatic

 

Therapeutic Considerations:Significant CNS effects, CNS depression, rare cases of psychosis when taken during pain/anxiety; Can be delivered via transdermal patch placed behind ear (Trans Scop patches); Subject to abuse (produces euphoria)

Term
Drug:Homatropine
Definition

 

 

Mech of Action:Tertiary amine antimuscarinic (Semi-synthetic) for Ophthalmic use Quaternary form: GI

 

Clinical Applications:Mydriatic and cycloplegia (loss of accommodation) for refraction

 

Serious and Common Adverse Events:Increased IOP --> Systemic anticholincergic effects with repeated dosing; Mydriatic and cyclopegia (loss of accommodation) for refraction; Acute inflammatory conditions for the uveal tract; Local irritation, vascular congestion, edema, exudate, eczema

 

Contraindications:Narrow-angle glaucoma (Mydriatic)

 

Therapeutic Considerations:shorter duration of action than atropine (12 to 24 hours)

Term
Drug:Tropicamide
Definition

 

 

Mech of Action:Semisynthetic antimuscarinic

 

 Clinical Applications:Mydriatic for fundus examination, Cycloplegia for refraction

 

Serious and Common Adverse Events:Increased IOPcardiovascular events and death (use w/ hydroxyamphetamine)

 

Contraindications: Narrow-angle glaucoma (Mydriatic)

 

Therapeutic Considerations:Cycloplegia may require 2 doses and study w/in 30 minutes due to drug elimination: Shorter duration of action than atropine (15 to 60 minutes)

Term
Drug:Ipatropium
Definition

 

 

 Mech of Action:quaternary muscarinic antagonist. block all subtypes of muscarinic receptors

 

 Clinical Applications:chronic obstructive pulmonary disease, Asthma, FDA approved for perennial and common cold–associated rhinorrhea

 

Serious and Common Adverse Events:Paralytic ileus, anaphylaxis, oropharyngeal edema Abnormal taste in mouth, xerostomia (nasal spray)

 

Contraindications: hypersensitivity to ipratropium or tiotropium

 

Therapeutic Considerations:More effective than β-adrenergic agonists in the treatment of COPD, but less effective in treating asthma.Lack action in the CNS. Administered as an aerosol/solution for inhalation:Does not produce adverse effects on mucociliary clearance. Lasts for 4-6 hours

Term
Drug:Tolterodine
Definition

 

 Mech of Action:potent tertiary amine muscarinic antagonist =synthetic substitute of atropine. selectivity for urinary bladder. It is able to lower the intravesicular pressure and increase capacity and to reduce the frequency of contractions by antagonizing the parasympathetic bladder control.

 

Clinical Applications:This is used to treat hyperreflexic and overactive bladder disease. Also treats urge incontinence.

 

Serious and Common Adverse Events:dry mouth and eyes (limit the tolerability) constipation, diarrhea, nausea, application-site erythema pruritus ( itchy rash)

 

Contraindications: Narrow-Angle Glaucoma

 

Therapeutic Considerations:nonspecific muscarinic receptor antagonist. This may cause less dry mouth than oxybutin.

Term
Drug:Oxybutynin
Definition

 

 

Mech of Action:This is a tertiary amine that is a muscarinic antagonist

 

Clinical Applications:treats hyperreflexic and overactive urinary bladder disease as well as urge incontinence

 

Serious and Common Adverse Events:constipation, diarrhea, nausea, dry mouth, and application-site erythema pruritus

 

 Contraindications:Narrow Angle Glaucoma

 

Therapeutic Considerations:nonspecific muscarinic receptor antagonist.used to overcome the dry mouth and eyes of other medications had such as tolterodine, tropsoum chloride, darifenacin, solifenacin, and flavoxate.The transdermal system delivers 3.9mg a day & has a lower incidence of side effects than the oral immediate or the extended-release preps

Term
Drug:Trospium
Definition

 

Mech of Action:A QUATERNARY AMINIE muscarinic antagonist. Lower intravesicular pressure and increases capacity by reducing the smooth muscle tone of the bladder. Reduces the frequency of contractions by antagonizing parasympathetic bladder control.

 

Clinical Applications:Treatement of overactive urinary bladder disease

 

Serious and Common Adverse Events:dry mouth and eyes which lead to a decline in patient acceptance. Also constipation, diarrhea, nausea, application-site erythema, pruritus.

 

Contraindications: Narrow-angle glaucoma

 

Therapeutic Considerations:*A synthetic substitute of atropine. nonspecific muscarinic receptor antagonists

Term
Drug:Solifenacin
Definition

 

 

Mech of Action:A selective M3 receptor antagonist. Blocks Ach binding to muscarinic cholinergic receptors at neuroeffector sites.

 

Clinical Applications:Treatment for overactive bladder

 

Serious and Common Adverse Events:Common: dry mouth and eyes, constipation, diarrhea, nausea, application-site erythma, pruritus

 

Contraindications: Narrow-angle glaucoma

 

Therapeutic Considerations solifenacin are selective M3 receptor antagonists  solifenacin may cause less dry mouth/constipation

Term
Drug:Flavoxate
Definition

 

Mech of Action:A synthetic TERTIARY AMINE muscarinic antagonist. Antispasmodic agent. It prevents urinary tract smooth muscle spasm

 

 Clinical Applications:Treatment of overactive bladder or excessive urination, painful urination (dysuria), urgency, incontinence.

 

 Serious and Common Adverse Events:Common: nausea, vomitting, dry mouth, nervousness

 

Contraindications: gastrointestinal obstruction, obstruction uropathies, achalasia (inability of relaxation by circular muscle).

 

 Therapeutic Considerations:Antispasmodic

Term
Drug:Hyoscyamine
Definition

 

 

Mech of Action: muscarinic receptor antagonist.  belladonna alkaloid, which can reduce tone and motility of GI tract when administered in maximal tolerated doses; Expected to be useful in conditions involving excessive smooth muscle contraction (this often may not be the case; M3-selective

 

 Clinical Applications:Peptic ulcer disease Irritable bowel syndrome, hypermotility disorders, infant colic (Used in a wide variety of conditions known or supposed to involve irritable bowel and increased tone (spasticity) or motility of the GI tract. )

 

Serious and Common Adverse Events:Serious: Increased intraocular pressure, tachycardia, palpitations Common: Dryness of the mouth, urinary hesitancy and retention, blurred vision, mydriasis

 

Contraindications: Narrow-angle glaucoma, myasthenia gravis

 

Therapeutic consideration: Longer duration of action than dicyclomine

Term
Drug:benztropine
Definition

 

 

 Mech of Action:tertiary-amine muscarinic receptor antagonist Selectively

 

 Clinical Applications:Adjunt for Parkinsonism. (It is used to treat parkinsonism and extrapyramidal side effects of antipsychotic agents.) It only improves tremor and dystonia symptoms, not rigidity or bradykinesia.

 

Serious and Common Adverse Events:Serious: Angle-closure glaucoma, increased intraocular pressure, psychosis, hyperpyrexia, paralytic ileus Common: Dizziness, blurred vision, nervousness, nausea, xerostomia, urinary retention

 

Contraindications: Narrow-angle glaucoma; Younger than 3 years

 

Therapeutic Considerations:Benztropine (and Trihexyphenidyl) reduce tremor more than bradykinesia and are therefore effective in treating patients for whom tremor is the major clinical manifestation of Parkinson's disease; May worsen dementia and cognitive impairment in the elderly.

Term
Drug:Trihexyphenidyl
Definition

 

 

Mech of Action:tertiary-amine muscarinic receptor antagonist. Mech: Selective. VERY similar to Benztropine.

 

Clinical Applications:Adjunt for Parkinsonism. (It is used to treat parkinsonism and extrapyramidal side effects of antipsychotic agents.) It only improves tremor and dystonia symptoms, not rigidity or bradykinesia.

 

Serious and Common Adverse Events:Serious: Angle-closure glaucoma, increased intraocular pressure, psychosis Common: Dizziness, blurred vision, nervousness, nausea, xerostomia, urinary retention

 

Contraindications: Narrow-angle glaucoma; Younger than 3 years; Tardive dyskinesias 

 

 Therapeutic Considerations:Trihexyphenidyl (and benztropine) reduce tremor more than bradykinesia and are therefore effective in treating patients for whom tremor is the major clinical manifestation of Parkinson's disease; May worsen dementia and cognitive impairment in the elderly

Term
Drug:Glycopyrrolate
Definition

 

 

Mech of Action:muscarinic antagonist that inhibits the acetylcholine activity on smooth muscles and structures innervated by postganglionic nerves resulting in a decreased volume and acidity of gastric secretions. Glycopyrrolate is employed orally to inhibit gastrointestinal motility and used parenterally to block the effects of vagal stimulation during anesthesia and surgery.

 

Clinical Applications:Peptic ulcer disease; surgically-induced or vagally-induced bradycardia

 

 Serious and Common Adverse Events:Cardiac arrhythmia, malignant hyperthermia, anaphylaxis, seizure Constipation, xerostomia, urinary retention, decreased sweating

 

Contraindications: Gastrointestinal obstruction Narrow-angle glaucoma

 

Therapeutic Considerations:Alternative or additive agents to standard peptic ulcer disease therapies. Methscopolamine and glycopyrrolate have delayed but measurable CNS and cognitive anticholinergic effects.

Term
Drug:Methscopolamine
Definition

 

 

Mech of Action: quaternary ammonium derivative of scopolamine that exerts anticholinergic effects (muscarinic antagonist), which include reducing the volume and total acid content of gastric secretion, inhibiting gastrointestinal motility and salivary secretion, dilation of the pupil and blocking accommodation that results in blurring of vision.

 

Clinical Applications:Pepti ulcer disease; Adjunct

 

 Serious and Common Adverse Events:Cardiac arrhythmia, malignant hyperthermia, anaphylaxis, seizure Constipation, xerostomia, urinary retention, decreased sweating

 

Contraindications: Gastrointestinal obstruction Narrow-angle glaucoma

 

Therapeutic Considerations:Alternative or additive agents to standard peptic ulcer disease therapies. Methscopolamine has delayed but measurable CNS and cognitive anticholinergic effects. Lacks the central actions of scopolamine. Other therapeutic considerations include: less potent than atropine and is poorly absorbed, action is more prolonged than atropine, usual oral dose is 2.5 mg and acts for 6 to 8 hours.

Term
Drug:Tiotropium
Definition

 

 

Mech of Action:Inhalation-Local: Tiotropium is a long-acting, muscarinic antagonist: anticholinergic. similar affinity to M1 to M5, but does show some selectivity towards M1 and M3, and lower affinity for M2. Dries the mucous membranes of the respiratory tract and inhibit secretions of the nose, mouth, pharynx and bronchi, and thus dry the mucous. It exhibits pharmacological effects through inhibition of M3-receptors at the smooth muscle leading to bronchodilation, tachycardia and inhibition of secretion.

 

Clinical Applications:Chronic obstructive pulmonary disease, asthma

 

Serious and Common Adverse Events:Paralytic ileus, anaphylaxis, oropharyngeal edema Abnormal taste in mouth, xerostomia (nasal spray)

 

Contraindications: Hypersensitivity to ipratropium or tiotropium

 

 Therapeutic Considerations:Hypersensitivity to ipratropium or tiotropium

Term
Drug:Methacholine
Definition

 

 

Mech of Action:Beta-methyl homolog of acetylcholine that induces bronchoconstriction by stimulating the nerve endings of the the vagus nerves. It resists inactivation by nonspecific ACHE or pseudocholineesterase.

 

Clinical Applications:Diagnosis of Asthma

 

Serious and Common Adverse Events:Gastrointestinal:Constipation (4%), Xerostomia (12% to 16%

 

Contraindications: Recent heart attack or stroke Aortic aneurysm Uncontrolled hypertension

 

Therapeutic Considerations:

Term
Drug:Dicyclomine
Definition

 

 

Mech of Action:anticspasmodic and anticholinergic agent (alleviates smooth muscle spasm in GI)

 

 Clinical Applications:Irritable bowel syndrome, minor diarrhea

 

Serious and Common Adverse Events:Respiratory:Pharyngitis (7% to 9%), Sinusitis (3% to 11%), Upper respiratory infection (41% to 43%)

 

Contraindications: Narrow-angle glaucoma, gastrointestinal obstruction, urinary obstruction, myasthenia gravis

 

Therapeutic Considerations:Short half life (1.8 hours) but action lasts up to 6 hours

Term
Drug:Acetylcholine
Definition

 

 

 Mech of Action:interferes w/ transmission of nerve impulses at cholinergic sites.

 

 Clinical Applications:Produce miosis during ophthalmic surgery

 

Term
Drug:Metoclopramide
Definition

 

 

Mech of Action:Muscarinic Receptor sensitizer - acts as a dopamine antagonist

 

Clinical Applications:GI motility disorders (gastiric stasis, gastroesophageal reflux disorder), prevention of chemotherapy-induced emesis

 

Serious and Common Adverse Events:extrapyramidal effects (Parkinson's like symptoms because of lack of DA. Gastrointestinal:Bowel obstruction

 

Contraindications: pheochromocytoma, seizure disorders, patients taking antipsychotic drugs possibly causing (phenothiazines, butyrophenones

 

Therapeutic Considerations:chronic use of metoclopramide has been linked to tardive dyskinesia

Term
Drug:Propantheline
Definition

 

 

Mech of Action:muscarinic receptor antagonist

 

Clinical Applications:hyperreflexive and overactive bladder - urge incontinence

 

Serious and Common Adverse Events:Immunologic:Hypersensitivity reaction, immediate

 

Contraindications: narrow angle glaucoma

 

Therapeutic Considerations:it is a NONSPECIFIC muscarinic receptor antagonist - High doses produce the symptoms of ganglionic blockade - toxic doses block the skeletal neuromuscular junction - Propantheline bromide is the widley used form

Term
Drug:Mepenzolate
Definition

 

 

Mech of Action:muscarinic receptor antagonist

 

Clinical Applications:Peptic Ulcer Disease Serious and

 

Common Adverse Events:Increased intraocular pressure, tachycardia, palpitations, dryness of mouth, urinary hesitancy and retention, blurred vision,mydriasis

 

Contraindications: Narrow angle glaucoma, myasthenia ravis, intestinal atony of the elderly or debilitated patients.

 

 Therapeutic Considerations:Diminishes gastric acid and pepsin secretion and also suppresses spontaneous contractions of the colon.

Term
Drug:Carbachol
Definition

 

 

Mech of Action:muscarinic agonist

 

Clinical Applications:Glaucoma

 

Serious and Common Adverse Events:sweating, shivering, nausea, dizziness, increased frequency of urination, rhinits (oral formulations).

 

Contraindications: Acute iritis or glaucoma after cataract extraction. Narrow-angle (angle-closure) glaucoma.

 

Therapeutic Considerations:enhanced nicotinic action relative to other choline esters; cannot be used systemically because of its unpredictable nicotinic action at autonomic ganglia; topical application of carbachol to the cornea of the eye results in both papillary constriction (miosis) and decreased intraocular pressure.

Term
Drug:Echothiophate
Definition

 

 

Mech of Action:organophosphate AChE agent: quartarnary

 

 Clinical Applications:Advanced Glaucoma (open angle)

 

Serious and Common Adverse Events:uveitis, brow ache, blurred vision

 

 Contraindications: may be implicated in development of cataracts

 

Therapeutic Considerations:Only organophosphate compound used clinically; limited to opthalmic administration; quaternary ammonium compound

Term
Drug:Physostigmine
Definition

 

 

Mech: "Reversible" Carbamate AChE Inhibitor

 

Clinical applications: Treatment of glaucoma; anticholinergic poisoning --> useful in the treatment of intoxication by atropine and several drugs with anticholinergic side effects; as well as the treatment of Friedreich's or other inherited ataxias; Adie (or tonic pupil) syndrome -->Low concentrations of physostigmine decrease the blurred vision and pain; potentially useful in reversing the central anticholinergic syndrome

 

Common and serious Adverse effects:Seizure, bronchospasm, cardiac arrhythmia, bradycardia, cardiac arrest Hypotension or hypertension, salivation, lacrimation, diaphoresis, vomiting, diarrhea, miosis

 

Contraindications: Mechanical intestinal or urinary obstruction Concomitant choline ester or depolarizing neuromuscular blocker use Cardiovascular disease

 

Therapeutic considerations:Absorbed readily from the GI tract, subcutaneous tissues and mucous membranes; May result in systemic effects --> Pressure on the inner canthus can prevent absorption from the nasal mucosa; Parenterally administered physostigmine --> Largely destroyed within 2 hours; Renal excretion plays only a minor role in its elimination; Oximes are not effective in antagonizing more rapidly hydrolyzing carbamoyl ester inhibitors; may precipitate seizures

Term
Neostigmine
Definition

 

 

Mech: "Reversible" Carbamate Inhibitor: Direct cholinergic agonist effect at Nm receptors

 

Clinical applications: - Myasthenia Gravis: Urinary or gastrointestinal motility agent*, glaucoma, Atony of the detrusor muscle of the urinary bladder

 

Common and serious Adverse effects:Seizure, bronchospasm, cardiac arrhythmia, bradycardia, cardiac arrest Hypotension or hypertension, salivation, lacrimation, diaphoresis, vomiting, diarrhea, miosis

 

Contraindications:Mechanical intestinal or urinary (bladder) obstruction. Peritonitis. Viability of bowel?; bowel dysfunction from IBS. Concomitant choline ester or depolarizing neuromuscular blocker use. Cardiovascular disease

 

Therapeutic considerations:Quaternary amine; Longer acting  myas. gravis drug of choice; Equal or greater potency to physostigmine; Not effective against the skeletal muscle paralysis caused by succinylcholine

Term
Edrophonium
Definition

 

 

Mech: Reversible inhibition @ ACHE active center, Simple alcohol with Quaternary structure (limited to periphery).

 

Clinical applications:diagnosis of myasthenia gravis, Eaton-Lambert syndrome and other diseases of NMJ resulting in muscle weakness.Terminating attacks of paroxysmal supraventricular tachycardia (rapid heart rate that start in heart above the ventricles)

 

Common and serious Adverse effects:Seizure, bronchospasm, cardiac arrhythmia, bradycardia, cardiac arrest Hypotension or hypertension, salivation, lacrimation, diaphoresis, vomiting, diarrhea, miosis

 

Contraindications:mechanical, intestinal or urinary obstruction. Concomitant choline ester or depolarlizing NM blocker use CV disease

 

 Therapeutic considerations:Short half life, renally eliminated, Limited volume of distribution. When the edrophonium test is performed cautiously the Dose is limited to 2 mg and with respiratory resuscitation available. decrease in strength= cholinergic crisis. Improvement signifies myasthenic weakness

Term
Donepezil (aricept) 
Definition

 

Mech: A REVERSIBLE anticholinesterase. Binds to the active center of AChE. Hydrophobic enough to readily cross BBB to cause inhibition in CNS.

 

 Clinical applications: Treatement for mild to moderate Alzheimer's disease, dementia

 

Common and serious Adverse effects:Common: nausea, diarrhea and vomitting, cramps, anorexia, vivid dreams. Side effects attributable to excessive cholinergic stimulation. *Well tolerated in single daily doses.

 

Contraindications:Treatment-associated liver function test abnormalties (contraindication for tacrine)

 

Therapeutic considerations:Long duration of action due to its lipophilicity and high affinity for AChE. , donepezil,=modest symptomatic benefits in Alzheimer's disease .

Term
Tacrine
Definition

 

 

Mech: Reversible Noncovalent AChE Inhibitor; binds to enzyme's active site (choline subsite).

 

 Clinical applications: Mild to moderate Alzheimer's disease; Dementia. (Works by enhancing concentrations of cholinergic NTs in the CNS).

 

 Common and serious Adverse effects:Common: Diarrhea, nausea, vomiting, cramps, anorexia, vivid dreams

 

Contraindications:Treatment-associated liver function test abnormalities (contraindication for tacrine) // Higher incidence of hepatotoxicity limits utility of Tacrine (30% of pts receiving low doses in 3 months: ALT 3x normal but return to normal upon discontinuation of drug; liver function values return to normal in 90% of pts; it also has other side effects typical of AChE inhibitors).

 

Therapeutic considerations:Tacrine =modest symptomatic benefits in Alzheimer's . : Tacrine (and donepezil) have high affinities for AChE; more hydrophobic & readily cross BBB (inhibits AChE in CNS); longer duration of action (due to partitioning into lipid and higher affinities for AChE).

Term
Rivastigmine
Definition

 

 

 Mech: Reversible AChE inhibitor, long-acting carbamoylating inhibitor.and buytylesterase!!!!!!!!!!!!!

 

 Clinical applications: Mild to moderate Alzheimer's disease Dementia.

 

Common and serious Adverse effects:Diarrhea, nausea, vomiting, cramps, anorexia, vivid dreams

 

Contraindications:

 

Therapeutic considerations:Carbamoylating inhibitor with high lipid solubilities. Readily crosses the blood–brain barrier. Longer duration of action.

Term
Pyridostigmine
Definition

 

 

Mech: Reversible carbamate inhibitor

 

 Clinical applications: Myasthenia gravies, pretreatment of pyridostigmine reduces the incapacitation and mortality associated with nerve gas poisoning

 

Common and serious Adverse effects:Seizure, bronchospasm, cardiac arrhythmia, bradycardia, cardiac arrest, hypo or hypertension, SLUD, diaphoresis.

 

Contraindications:Mechanical intestinal or urinary obstruction. Commit ant choline ester or depolarizizing neuromuscular blocker use for cardiovascular diseases.

 

Therapeutic considerations:Available for oral and parental. Also sustained release tablets. Duration of action is 3-6 hrs.

Term
Galantamine
Definition

 

 

Mech: AChE inhibitor

 

Clinical applications:mild to moderate alzheimer's disease / dementia

 

Common and serious Adverse effects:diarrhea, nausea, vomiting, cramps, anorexia, vivid dreams

 

Contraindications:

 

Therapeutic considerations:produces modest syptomatic benefits in alzheimer's disease and also acts as a non potentiating ligand of nicotinic receptors

Term
Demecarium
Definition

 

 

 Mech: AChE inhibitor

 

Clinical applications: open angle glaucoma

 

Common and serious Adverse effects:allergic reaction, admonial cramps or diarrhea, burning, stinging or red eyes, headached or brow ache, decreased vision in poor light

 

Contraindications:pregnancy; active uveal inflammation; angle-closure glaucoma

 

Therapeutic considerations:

Term
Ambenonium
Definition

 

 

 Mech: AChE inhibitor

 

 Clinical applications: Myasthenia gravies

 

Common and serious Adverse effects:Nausea, vomiting, diarrhea, abdominal cramps, increased saliva/mucus, decreased pupil size, increased urination, or increased sweating may occur

 

Contraindications:Parkinson Symptoms, Asthma, Stomach or Intestine Blockage, Urinary Tract Blockage

 

Therapeutic considerations:

Term
Pralidoxime
Definition

 

 

Mech: Cholinestrase Reactivator

 

Clinical applications: Moderate or severe intoxication with an organophosphorus anti-ChE agent

 

 

Term
Procaine
Definition

 

 

Mech: block Na voltage gated channels

 

 Clinical applications: major: used in infiltration anaesthetics and dental procedures; minor: diagnostic nerve blocks

 

Common and serious Adverse effects:Cardiac arrest and hypotension from

 excessive systemic absorption, CNS depression or 

excitation, respiratory arrest Contact dermatitis (same as 2-chloroprocaine)

 

Contraindications:same a (2-chloroprocaine) Use epidural anesthesia with extreme caution in patients with neurological disease, spinal deformities, septicemia, or severe hypertension

 

Therapeutic considerations:procaine has a low hydrophobicity, therefore rapid drug removal from administration site (circulation), low potency (at administration site) and short half life.

Term
2-Chloroprocaine
Definition

 

 

Mech: Ester-linked local anesthetics

 

Clinical applications: Popular as an obstetric anesthetic --> Given epidurally just before delivery to control pain

 

Common and serious Adverse effects:Cardiac arrest and hypotension from excessive systemic absorption, CNS depression or excitation, respiratory arrest Contact dermatitis

 

Contraindications:Use epidural anesthesia with extreme caution in patients with neurological disease, spinal deformities, septicemia, or severe hypertension

 

Therapeutic considerations:Parenteral duration 15 to 30 minutes Parenteral duration 30 to 90 minutes with epinephrine

Term
Tetracaine
Definition

 

 

Mech: Inhibit voltage-gated sodium channels in excitable cell membranes

 

Clinical applications: topical anesthesia; spinal anesthesia

 

Common and serious Adverse effects:Cardiac arrest and hypotension from excessive systemic absorption, CNS depression or excitation, respiratory arrest Contact dermatitis **AND: drug-induced keratoconjunctivitis

 

Contraindications:localized infection at proposed site of topical application

 

Therapeutic considerations:High hydrophobicity confers longer duration of action and higher potency: tetracaine is more potent than lidocaine and procaine; Do not inject large doses in patients with heart block

Term
Cocaine
Definition

 

 

Mech: NET inhibitor - prevents NE reuptake --> promotes excitatory adrenergic neurotransmission

 

Clinical applications: Local anesthetic: mucosal and opthalmic; Diagonisis of Horner's syndrome pupil

 

Common and serious Adverse effects:accelerates coronary atherosclerosis, tachycardia, seizure; CNS depression or excitation, anxiety

 

Therapeutic considerations: Medium potency and duration; Vasoconstriction, toxicity, and euphoria limit value as a local anesthetic

Term
Lidocaine
Definition

 

Mech: prototypical ester-linked and amide-linked local anesthetics. Most commonly used LA. Blocks sodium channels in cardiac myocytes.Moderate hydrophobicity keeps drug near the area of entry- Amide linkage prevents drug degradation by esterases

 

Clinical applications: Infiltration anesthesia Peripheral nerve block Epidural, spinal, and topical anesthesia Class I antiarrhythmic

 

Common and serious Adverse effects:CNS Excitation:Drowsiness, tinnitus, twitching and seizures - CNS depression and cardiotoxicity occur at high plasma levels

 

Contraindications:Hypersensitivity to amide-linked local anesthetics

 

Therapeutic considerations:Rapid rate of onset, Extremely low incidence of allergic reaction, more resistant to clearance and have longer durations of action. Difficult to block Aδ-fibers without also blocking Aγ- motor fibers.Insoluble in water and poorly absorbed into the circulation (decreases the likelihood of systemic toxicity).initially causes vasoconstriction,later produces vasodilation.Moderately potent due to hydrophobicity allowing channel binding.Vasoconstrictive effects of co-administered epinephrine=Extends lidocaine's duration of action significantly

Term
Prilocaine
Definition

 

 

Mech: Similar to lidocaine= Exception: has vasoconstrictive activity

 

Clinical applications: Dental infiltration anesthesia and nerve

 

Common and serious Adverse effects:CNS Excitation:Drowsiness, tinnitus, twitching and seizures - CNS depression and cardiotoxicity occur at high plasma levels

 

Contraindications:Hypersensitivity to amide-linked local anesthetics

 

Therapeutic considerations:Does not require concurrent administration of epinephrine= Good choice for patients when epinephrine is contraindicated

Term
Bupivacaine
Definition

 

 

Mech: Blocks sensory impulses without significant motor block.

 

Clinical applications: Commonly used for infiltration anesthesia, spinal, regional epidural and peripheral nerve block. Used in dentistry for lengthy procedures and postoperative pain. Dilute epidural can be used for labor pain relief.

 

Common and serious Adverse effects:Cadiotoxicity reported at high concentrations. CNS excitation.

 

Contraindications:Local infection at the proposed site of spinal anesthesiaContraindicated for use in spinal anesthesia in the presence of septicemia, severe hemorrhage, shock, or arrhythmias such as complete heart block

 

Therapeutic considerations:Highly hydrophobic, high potency, long duration of action. Cardiotoxicity at higher concentrations limits its use. The R-enantiomer and S-enantiomer have different affinities for the sodium channel and, therefore, different cardiovascular effects; the S-enantiomer is levobupivacaine. High hydrophobicity results in low plasma concentration and large Vd and therefore eliminated slower. (gets into more of the tissues)

Term
Articaine
Definition

 

 

Mech: Amide-linked local anesthetic; Mech: Inhibit voltage-gated sodium channels in excitable cell membranes

 

Clinical applications:Dental anesthesia; Epidural, spinal, and regional anesthesia

 

Common and serious Adverse effects:CNS excitation Contraindications:Infection at site of injection (especially lumbar puncture sites); Shock

 

Therapeutic considerations:current clinical application largely in dentistry. Articaine is rapidly metabolized (partially metabolized in plasma by cholinesterases; also metabolized in liver), which can min. potential toxicity.

Term
Levobupivacaine
Definition

 

Mech: Local anesthetic that acts by blocking the conduction and generation of nerve impulses probably increasing threshold. S-enantiomer of Bupivacaine.

 

Clinical applications: Infiltration, regional, epidural, and spinal anesthesia. Sympathetic nerve block.

 

Common and serious Adverse effects:Compared to bupivacaine, levobupivacaine causes less vasodilation and has a longer duration of action.

 

Contraindications:Local infection at the proposed site of spinal anesthesia Contraindicated for use in spinal anesthesia in the presence of septicemia, severe hemorrhage, shock, or arrhythmias such as complete heart block.

 

Therapeutic considerations:Highly hydrophobic, high potency, long duration of action Cardiotoxicity at higher concentrations limits its use The R-enantiomer and S- enantiomer have different affinities for the sodium channel and, therefore, different cardiovascular effects; the S-enantiomer is levobupivacaine.

Term
Ropivacaine
Definition

 

 

Mech: Inhibit voltage gated sodium channels in excitable cell membranes.

 

Clinical applications: Management of acute pain (postoperative or labor ) local or regional anesthesia for surgery.

 

Common and serious Adverse effects:Hypotension, CNS excitation

 

Contraindications:Hypersensitivity

 

Therapeutic considerations:May have less cardio toxicity than Bupivacaine

Term
Lidocaine and Prilocaine
Definition

 

 

Mech: Local anesthetic action occurs by stabilization of neuronal membranes and inhibiting the ionic fluxes required for the initiation and conduction of impulse


Clinical applications: venipuncture, arterial cannulation, and lumbar puncture and kid's dental procedures for injections

 

 Therapeutic considerations:delivered topically as a cream or patch; higher concentration of local anesthetic per drop contacting skin

Term
Tetracaine, Adrenalin, Cocaine (TAC)
Definition

 

Mech: Topical anesthetic

 

Clinical applications: Prior to strutting small cuts

 

Common and serious Adverse effects:Cocaine dependence 

Term
Nicotine
Definition

 

 

Mech: agonist at Nn and Nm: first stimulate ganglia and then block due to depolarization. Tricky MOA since it can stimulate or inhibit systems somewhat randomly.

 

Clinical applications:smoking cessation

 

Contraindications:Increased GI activity, nausea, vomiting, diarrhea, increase bp. High doses: seizures, GI and CVD risk factor

 

Therapeutic considerations:additive with CNS stimulants.

Term
Succinylcholine
Definition

 

Mech: depolarizing blocker: agonist at nicotinic ACh receptors, especially at nm junctions. Phase I and Phase II nm blockade dependent on drug activity time: see table 3, pg 10. Depolatization may also stimulate ganglionic receptors: nicotinic ACh and cardiac muscarinic ACh

 

Clinical applications: rare: placement of tracheal tube at start of anesthetic procedure; control of muscle contraction in status epilepticus.

 

Common and serious Adverse effects:arrhythmias, hyperkalemia, transient increased intra-abdominal and intraocular pressure, postoperative muscle pain.

 

Contraindications:patients with: nontraumatic rhabdomyolysis, ocular lacerations, spinal cord injuries wth paraplegia or quadriplegia, muscular dystrophies; should not be used after competitive blockade from neostigmine (additive blockage results)

 

Therapeutic considerations:not indicated for children under 8. Short mechanism of action (rapid metabolism by plasma cholinesterases, normal duration of effect 5-8 minutes.

Term
Pancuronium
Definition

 

 

Mech: Competitive antagonist at nACh receptors especially at neuromuscular junctions; Ammonio steroid; competitive Neuromuscular Blocking Agent; Does blocks muscarinic receptors--> Manifested primarily in vagal blockade and tachycardia; Prevents depolarization by ACh; Weak block of cardiac muscarinic ACh receptors

 

Clinical applications: Prolonged relaxation of surgical procedures; Relaxation of muscles to facilitate intubation; Relaxation of respiratory muscles to facilitate mechanical ventilation;Causes flaccid paralysis Can cause histamine release with hypotension

Common and serious Adverse effects:Cardiovascular (increased arterial pressure, heart rate, cardiac output), salivation, apnea

 

Therapeutic considerations:history of persistent blockade and difficulty in complete reversal after surgery; Long duration; time of onset 4-6 minutes;intermediate duration of action; mode of elimination--Renal; Induces virtually no histamine release; shows less ganglionic blockade at common clinical doses; Duration about 120 to 180 min

Term
Tubocurarine
Definition

 

Mech: competitive Neuromuscular Blocking Agents; Natural alkaloid (cyclic benzylisoquinoline); block the binding of ACh; Diminish progressively the amplitude of the excitatory postjunctional EPP --> Insufficient to initiate the propagated muscle action potential; Reduces the frequency of channel-opening events; Does not affect the conductance or duration of opening for a single channel

 

Clinical applications: Prolonged relaxation for surgical procedures Superseded by newer nondepolarizing agents

 

Common and serious Adverse effects:Results in a fall in blood pressure and tachycardia

 

Therapeutic considerations:Long duration; time of onset 4-6 minutes; Renal elimination; liver clearance; clinical duration 80-120 minutes; Inability to penetrate the blood–brain barrier

Term
Vecuronium
Definition

 

 

Mech: Ammonio steroid: non-depolarizing neuromuscular blocker; Competitive antagonist at nACh receptors esp. at neuromuscular junction

 

Clinical applications: Prolonged relaxation of surgical procedures; Relaxation of muscles to facilitate intubation; Relaxation of respiratory muscles to facilitate mechanical ventilation

 

Common and serious Adverse effects: Apnea, skeletal muscle weakness

 

 Therapeutic considerations:intermediate duration; competitive;Time of onset 2-4 min; Duration 60-90 min.; less tendency to release histamine and has greater selectivity than some other neuromuscular blocking agents; metabolized in liver

Term
Rocuronium
Definition

 

 

Mech: amino steroid.Competitive antagonist at nACh receptors esp @ neuromuscular junctions

 

Clinical applications: Rapid induction anesthesia.Relaxing the laryngeal and jaw muscles to facilitate tracheal intubation

 

Common and serious Adverse effects:Like tubocurarine no histamine release and minimal antimuscarinic effects

 

Contraindications:Prolonged relaxation of surgical procedures.Relaxation of muscles to facilitate intubation Relaxation of respiratory muscles to facilitate mechanical ventilation

 

Therapeutic considerations:metabolized by liver,more selective than pancuronium. Duration about 30 to 60 min.Adverse effects: Like cisatracurium tendency to release histamine after intradermal or systemic injection. Intermediate duration of action.

Term
Mivacurium
Definition

 


Mech: Neuromusclar blocking agent. Competitive antagonist at the NMJ


Clinical applications: Prolonged relaxation of surgical procedures. Relaxation of muscles to facilitate intubation (the introduction of a tube into a hollow organ or to keep tube open or restore its patency if obstructed). Relaxation of respiratory muscles to facilitate mechanical ventilation.

 

Common and serious Adverse effects:Flush, hypotension, rash, bronchospasm. Slight histamine release (unless administered rapidly). Devoid of antimuscarinic effects. Prevents depolarization by ACh. Causes flaccid paralysis. Can cause histamine release with hypotension. Weak block of cardiac muscarinic ACh receptors. 

 

Therapeutic considerations:Metabolized by plasma cholinesterases (butyrylcholinesterase) through hydrolysis. Also extremely sensitive to catalysis by plasma hydrolases. Therefore, it has the shortest duration of the nondepolarizing blockers with a duration of 12 to 18 minutes.

Term
Atracurium
Definition

 

 

Mech: Neuromuscular blocking agent. Competitive antagonist at NMJ nicotinicACh receptors.

 

Clinical applications: Prolonged relaxation of surgical procedures. Relaxation of muscles to facilitate intubation. Relaxation of respiratory muscles to facilitate mechanical ventilation.

 

Common and serious Adverse effects:Adverse effects: usually due to histamine release (flush, itching), prolonged apnea. Slight histamine release (unless administered rapidly). Devoid of antimuscarinic effects. Prevents depolarization by ACh. Causes flaccid paralysis. Can cause histamine release with hypotension. Weak block of cardiac muscarinic ACh receptors.

 

Therapeutic considerations:Not dependent on renal or hepatic function, therefore, both routes of elimination are functional in renal failure. Duration about 30-60 minutes. Renally eliminated. Metabolized by: 1) plasma esterases through hydrolysis of the ester, 2) spontaneous (Hofmann) degradation by cleavage of the benzylisoquinoline N-alkyl.

Term
Cisatracurium
Definition

 

 

Mech: Neuromuscular Blocking Agent- Competitive antagonist at nACh receptors especially at neuromuscular junctions. Effects: Like tubocurarine (Prevents depolarization by Ach; Causes flaccid paralysis; Can cause histamine release with hypotension) but only slight histamine release and devoid of antimuscarinic effects.

 

Clinical applications:Prolonged relaxation of surgical procedures; Relaxation of muscles to facilitate intubation; Relaxation of respiratory muscles to facilitate mechanical ventilation (Same as Atracurium)

 

Common and serious Adverse effects:Adverse effects: Prolonged apnea but less toxic & fewer adverse effects than atracurium

 

Therapeutic considerations:Not dependent on renal or hepatic function; Duration about 25–45 min; // Other info: Cisatracurium: 10 cis isomers (15% of atracurium). Benzylisoquinolines [-acrurium] (devoid of vagolytic & ganglionic blocking actions, show slight propensity for histamine release).

Term
Doxacurium
Definition

 

 

Mech:Competitive antagonist at nACh receptors especially at neuromuscular junctions. Like tubocurarine but only slight histamine release and devoid of antimuscarinic effects.

 

Clinical applications: Prolonged relaxation of surgical procedures. Relaxation of muscles to facilitate intubation Relaxation of respiratory muscles to facilitate mechanical ventilation.

 

Common and serious Adverse effects: Adverse effects: flush, prolonged muscle weakness.

 

 Therapeutic considerations:Renal elimination. Duration about 90 to 120 min

Term
Mecamylamine
Definition

 

 

Mech: Selectively antagonizes

 

Clinical applications: Hypertension in patients with acute aortic dissection.

 

Common and serious Adverse effects:Paralytic ileus, urinary retention, respiratory arrest, syncope, dyspepsia, orthostatic hypertension, Diplopia, sedation.

 

 Therapeutic considerations:Only therapeutic ganglionic blocker in US.

Term
Botulinum toxin A
Definition

 

 

Mech: muscle relaxant (cleaves SNAP-25 in NMJ to disrupt SNARE complex and prevent Ach release)

 

Clinical applications:flaccid paralysis of skeletal muscle; ocular conditions of strabismus and blepharospasm; hemifacial spasms adductor spasmodic dysphonia; oromandibular dystonia; cervical dystonia; lower esophageal sphincter and anal fissure spasms; cosmetic procedures

 

Therapeutic considerations:inhibition lasts week to months; requires new nerve sprouting

Term
Dantrolene
Definition


 

Mech: Blocks RyR1 Ca2+-release channels in the sarcoplasmic reticulum of skeletal muscle

 

 

Common and serious Adverse effects:Muscle weakness

 

 

Term
Drug: Prazosin
Definition

 

 

Mech: A reversible ALPHA-adrenergic ANTAGONIST. Relatively high affinity at ALPHA-2B and ALPHA-2C subtypes compared with alpha 2A receptors. Directly relaxes vascular smooth muscle. Causes vasodilation of veins and arterioles and a decrease in total peripheral resistance and blood pressure.

 

Clinical Application: Treatment of hypertesion and may be used for benign prostatic hyperplasia

 

SE: Dizziness

Term
Clonidine
Definition

 


Mech:Alpha 2 selective adrenergic AGONIST


Clinical Application: HTN, Used as sympatholytic to treat symptoms associated with drug withdrawal. Cancer pain


Common and Serious RXNS: Bradycardia caused by decreased sympathetic activity and increased vagal activity. Heart failure. hypotension. Dry mouth and sedation, constipation, dizziness


Therapeutic Consideration: receptor affinity: A2>a1>>>>>>beta

Term
Guanabenz
Definition

 

 

Mech:Centrally acts as an alpha 2 agonist


Clinical Application:HTN


Common and Serious RXNS:Bradycardia caused by decreased sympathetic activity and increased vagal activity. Heart failure. hypotension. Dry mouth and sedation, constipation, dizziness


Therapeutic Consideration:Seldomly used and have adverse effect profiles similar to that of clonidine

Term
Guanfacine
Definition

 

Mech: Centrally acts as an alpha 2 agonist(note- everything is the same as guanabenz)


Clinical Application:HTN


Common and Serious RXNS: Bradycardia caused by decreased sympathetic activity and increased vagal activity. Heart failure. hypotension. Dry mouth and sedation, constipation, dizziness


Therapeutic Consideration: Seldomly used and have adverse effect profiles similar to that of clonidine

Term
Methyldopa (alpha methyldopa)
Definition

 


Mech: Alpha methyldopa- this is a precursor prodrug to the alpha 2 agonist methylnorepinephrine. This is released by the adrenergic nerve terminal and acts presynaptically as an alpha 2 agonist. Results in decreased sympathetic outflow from the CNS


Clinical Application:HTN


Common and Serious RXNS: Bradycardia, heart failure, heptotoxicity. Autoimmune hemolytic anemic. Hypotension, constipation, xerstomia, sedation, dizziness.


Contraindications: MAO inhibitor therapy and active liver disease


Therapeutic Consideration:Not the first-line agent in the the treatment of HTN, but proved to be safer than other anithypertensive agents in pregnancy (drug of choice for pregnancy)

Term
Isoproterenol
Definition

 


Mech:Nonselective beta AGONIST. Lowers peripheral resistance and diastolic BP (b2 effect). Systolic bp remains unchanged or slightly increased (b1 effect). Positive inotrop (incre contractility) and Chronotrope(incr hrt rte)= CO is increased. Stimulates beta adrenergic activation activation of insulin secretion


Clinical Application:EmergenC treatment of arrhythmias (IV) Atropine-resistant hemodynamically significant bradycardi (IV) Heart Block and shock (IV) Bronchospasm (inhalation)


Common and Serious RXNS: often accompanied by unwanted cardiac side effects (Arrhythmias including ventricular fibrillation, cerebral hemorrhage, severe hypertension Headache, nervousness, tremor, hypertension, palpitations, tachycardia).



Contraindication: Tachycardia caused by digitalis intoxication. Angina pectoris


Therapeutic Consideration: Causes less hyperglycemia than epinephrine.receptors:(nonselective Beta agonist) B1=b2>>alpha. May be useful in treating patients with refractory bradycardia not responsibe to atropine and in treatment patients with beta antagonist overdose. do NOT administer to pnts w/ active coronary artery disease

Term
Metaproterenol
Definition

 

 

Mech: Beta-2 selective agonist. (Prototype Beta 2 selective agonist) Activates beta-adrenergic receptors. Causes relaxation of bronchial smooth muscle. Decreases airway resistance.


Clinical Application: Treatment for obstructive airway disease and acute bronchospasm, asthma, COPD


Common and Serious RXNS: Some cardiac effects. May cause skeletal muscle tremor. Tachycardia through stimulation of B1. Has similar side effects to Isoproterenol: arrhythmias including ventricular fibrillation, cerebral hemorrhage, severe hypertension, headache, nervousness, tremor, hypertension, palpitations, tachycardia


Contraindication: Hypersensitivity to isoetharine, terbutaline, albuterol, levalbuterol, pibuterol, or bitolterol


Therapeutic Consideration: Receptor Affinity: B2 >> B1 >>>> alpha. **Similar but newer agents such as terbutaline and albuterol bind to Beta 2 adrenergic receptors 200 to 400 times more strongly than to beta 1 receptors, and cause fewer cardiac effects than the less selective adrenergic agonists.

Term
Albuterol
Definition

 

 

Mech:Beta-2 selective agonist.Activates beta-adrenergic receptors. Causes relaxation of bronchial smooth muscle. Decreases airway resistance.


Clinical Application: Asthma, COPD


Common and Serious RXNS: Some cardiac effects. May cause skeletal muscle tremor. Tachycardia through stimulation of B1. Has similar side effects to Isoproterenol: arrhythmias including ventricular fibrillation, cerebral hemorrhage, severe hypertension, headache, nervousness, tremor, hypertension, palpitations, tachycardia


Contraindications:Hypersensitivity to isoetharine, terbutaline, metaproterenol, levalbuterol, pibuterol, or bitolterol


Therapeutic Consideration: Receptor Affinity: B2 >>> B1 >>>> alpha. **This is a newer agent which binds 200 to 400 times more strongly to Beta 2 adrenergic receptors than to beta 1 receptors therefore causes fewer cardiac effects than the less selective adrenergic agonists.

Term
Alpha methyltyrosine
Definition

 

 

Mech:structural analogue of tyrosine (inhibits NE synthesis via tyrosine hydroxylase

 

Clinical Application:HTN associated with pheochromocytoma

 

Common and Serious RXNS:orthostatic hypotension, sedation

 

CI:hypersensitivity to alpha-methyl tyrosine


Therapeutic Consideration:used rarely

Term
Guanethidine
Definition

 

 

Mech:displaced NE in sympathetic neuron vessicles

 

Clinical Application: HTN

 

Common and Serious RXNS:postural hypotension, kidney disease, apnea, fluid retention, dizziness, blurred vision, impotence

 

CI:MAOI therapy, heart failure, pheochromocytom

 

Therapeutic Consideration:inhibition of cardiac sympathetic nerves leads to reduced CO

Term
Guanadrel 
Definition

 

 

Mech: displaced NE in sympathetic neuron vessicles

 

Clinical Application: HTN

 

Common and Serious RXNS:postural hypotension, kidney disease, apnea, fluid retention, dizziness, blurred vision, impotence

 

CI:MAOI therapy, heart failure, pheochromocytoma

 

Therapeutic Consideration:inhibition of cardiac sympathetic nerves leads to reduced CO

Term
Amphetamine
Definition

 

 

Mech:displaces catecholamines from storage vesicles; weak inhibitor of MAO; blocks catecholamine reuptake by NET and DAT

 

Clinical Application:depression; narcolepsy; suppress appetite, ADHD

 

Common and Serious RXNS:hypertension, tachycardia(increasing the amount sent out sympathetic) , Gilles de la Tourett's syndrom, seizure, psychotic disorder with prolonged use. Restlessness, dysphoric mood, rebound fatigue, addiction potential loss of appetite, irritability, erectile dysfunction

 

CI: CVD, glaucoma, hyperthyroidism, MAOI therapy, severe HTN

 

Therapeutic Consideration:dependence and tolerance can occur.

Term
Methylphenidate
Definition

 

 

Mech:dependence and tolerance can occur.

 

Clinical Application:ADHD, depression, suppress appetite

 

Common and Serious RXNS:hypertension, tachycardia, Gilles de la Tourett's syndrom, seizure, psychotic disorder with prolonged use. Restlessness, dysphoric mood, rebound fatigue, addiction potential loss of appetite, irritability, erectile dysfunction

 

CI:CVD, glaucoma, hyperthyroidism, MAOI therapy, severe HTN

 

Therapeutic Consideration:dependence and tolerance can occur.

Term
PSE
Definition

 

 

Mech:INHIBITORS OF CATECHOLAMINE STORAGE Mechanism—Inhibit catecholamine storage in vesicles, resulting in short-term increase in release of catecholamines from the synaptic terminal but long-term depletion of available pool of catecholamines

 

Clinical Application:Nasal congestion --> used as an over-the-counter decongestant (Found in some cold remedies and appetite suppressants); Allergic rhinitis

 

Common and Serious RXNS: same as the shit above, not so much the appetite. 

 

CI:

 

Therapeutic Consideration: precursor to meth

Term
Cocaine
Definition

 

 

Mech:Inhibits the NE transporter, allowing released NE to remain in the synaptic cleft for a longer period of time; potentiates neurotransmissio at adrenergic synapses


Clinical Application: Mucosal and opthalmic local anesthetic; diagnosis of Horner's syndrome pupil

 

Common and Serious RXNS:Mucsoal and opthalmic local anesthetic; diagnosis of Horner's syndrome pupil

 

CI:

 

Therapeutic Consideration:Most important role is as an agent of abuse

Term
Amitriptyline
Definition

 

 

Mech:Inhibit NET-mediated reuptake of NE into presynaptic terminals (allows accumulation of NE in the synapitc cleft); also inhibit serotonin reuptake into presynaptic terminals

 

Clinical Application:TCA

 

Common and Serious RXNS:May cause postural hypotension; May cause sinus tachycardia

 

CI:

 

 

Therapeutic Consideration: main toxicity of TCA is arrhythmia of the heart. Really easy to OD on TCA, hard to give to ppl who are depressed. 

Term
Iproniazid
Definition

 

 

Mech:Non-selective MOAI, irrversible

 

Clinical Application: Depression

 

Common and Serious RXNS:tyramine reaction 

 

CI:

 

Therapeutic Consideration:

Term
Brofaromine
Definition

 

Mech:Reversible inhibitor of MAO-A; increasing catecholamine levels by blocking catecholamine degradation

 

Clinical Application: Depression

 

Common and Serious RXNS:This one you have to remember the tyramine, it wants you to party- but beer and wine 

 

Therapeutic Consideration:

Term
Moclobemide
Definition

 

Mech:Reversible MOAi; A-selective (RIMA); incr. [catecholamines] in synapse

 

Clinical Application:Depression

 

Common and Serious RXNS:(Some) Systemic tyramine toxicity (uncontrolled catecholamine release can induce a hypertensive crisis) but less than non-selective MAOi, fever associated w/ incr. muscle tone, leukopenia, hepatic failure, drug-induced lupus, worsening depression; Dizziness, somnolence, orthostatic hypotnsion, weight gain, increased liver aminotransferase level, orgasm disorder

 

CI: Concomitant use of sympathomimetic drugs, bupropion, buspirone, guanethidine, other MAOIs, serotonergic drugs, methyldopa, L-dopa, L-tryptophan, L- tyrosine, phenylalanine, CNS depressants, narcotics, dextromethorphan, excessive coffee or chocolate intake, foods with high tyramine content

Liver disease, Pheochromocytoma, Heart failure,
General anesthesia, local anesthesia with vasoconstrictors

 

Therapeutic Consideration:RIMAs displaced by high [tyramine], resulting in significantly more tyramine metabolism and thus less tyramine toxicity

Term
Methoxamine
Definition

 

 

Mech:alpha 1 agonist (increasing the peripheral resistance but then the baroreceptors comes into play)

 

Clinical Application:vasoconstrictor; HYPOTENSION, Shock

 

Common and Serious RXNS:Bradcardia (HR under 60 bpm), ventricular ectopic beat; HTN, vasoconstriction, nausea, HA, anxiety

 

CI:severe HTN

 

Therapeutic Consideration:very limited use in clinical treatment of shock

Term
PE
Definition

 

 

Mech:alpha 1 agonist

 

Clinical Application:vasoconstrictor/pressor; Oral/Topical Uses:NASAL DECONGESTANT, OPHTHALMIC HYPEREMIA (red eye); IV - HYPOTENSION (used in heart failure for ppl that do not respond to inotropes)

 

Common and Serious RXNS:Cardiac arrhythmia, HTN; HA, insomnia, nervousness, rebound nasal congestion

 

CI:not to be used w/ narrow angle glaucoma, severe HTN, or tachycardia;

 

Therapeutic Consideration:Rebound effect, headache (anything with messing with BV) can be seen w/ symptoms of nasal congestion (use of medication for more than 3 consecutive days - receptor up & down regulation)- this is the only one that can be use IV compared to oxymetalozine, tetrahydrazoline)

Term
Oxymetazoline (affrin)
Definition

 

 

Mech:alpha 1 agonist

 

Clinical Application:vasoconstrictor/pressor; Oral/Topical Uses:NASAL DECONGESTANT, OPHTHALMIC HYPEREMIA (red eye)

 

Common and Serious RXNS:Cardiac arrhythmia, HTN; HA, insomnia, nervousness, rebound nasal congestion

 

CI:not to be used w/ narrow angle glaucoma, severe HTN, or tachycardia;

 

Therapeutic Consideration:Rebound effect can be seen w/ symptoms of nasal congestion (use of medication for more than 3 consecutive days - receptor up & down regulation)

Term
Tetrahydrazoline (visine)
Definition

 

 

Mech:

 

Clinical Application:vasoconstrictor/pressor; Oral/Topical Uses:NASAL DECONGESTANT, OPHTHALMIC HYPEREMIA (red eye

 

Common and Serious RXNS:Cardiac arrhythmia, HTN; HA, insomnia, nervousness, rebound nasal congestion

 

CI:not to be used w/ narrow angle glaucoma, severe HTN, or tachycardia;

 

Therapeutic Consideration:Rebound effect can be seen w/ symptoms of nasal congestion (use of medication for more than 3 consecutive days - receptor up & down regulation)

Term
Labetalol
Definition

 

 

Mech: Nonselective β- and α1-Antagonists (blocks α1-, β1-, and β2-receptors). Labetalol *also acts as a weak partial agonist at β2-receptors* (has a 5- to 10-fold greater effect as a β-blocker). It causes a decrease in blood pressure (α1-receptor blockade results in vasodilation and β1-blockade prevents a reflex sympathetic increase in heart rate). Mech: Block β-adrenergic receptors. Selectivity: β1 = β2 > α1 > α2

 

Clinical Application:Hypertension and Angina

 

Common and Serious RXNS:Same as propranolol (S: Bronchospasm, atrioventricular block, bradyarrhythmia; C: Sedation, decreased libido, mask symptoms of hypoglycemia, depression, dyspnea, wheezing). Additionally, labetalol can cause hepatotoxicity.

 

CI:Same as propranolol (Bronchial asthma or chronic obstructive pulmonary disease; Cardiogenic shock; Uncompensated cardiac failure; Second- and third-degree AV block; Severe sinus bradycardia).

 

Therapeutic Consideration:Labetalol blocks α1-, β1-, and β2-receptors. *Labetalol may cause liver damage!* (Liver function tests must be monitored)

Term
Salmeterol
Definition

 

 

Mech:Beta-2 selective agonist. Causes relaxation of bronchial smooth muscle. Decreases airway resistance. Long-acting lasting about 12 hours

 

Clinical Application:Asthma, COPD.

 

 

Common and Serious RXNS:Some cardiac effects. May cause skeletal muscle tremor. Tachycardia through stimulation of B1. Has similar side effects to Isoproterenol: arrhythmias including ventricular fibrillation, cerebral hemorrhage, severe hypertension, headache, nervousness, tremor, hypertension, palpitations, tachycardia.

 

CI:Hypersensitivity to formoterol.

 

Therapeutic Consideration:Due to its lipophilic side chains that resist degradation, salmeterol is long-acting β2 agonists (LABAs) with a duration of action lasting 12 to 24 hours Salmeterol should NOT be used for acute asthma flares due to its slow onset of action.

Term
Epinephrine
Definition

 

 

Clinical Application:Epinephrine synthesis predominates in adrenal medullary cells. Rapid onset and a brief duration of action.

 

Common and Serious RXNS:Bronchospasm Hypersensitivity reaction, anaphylactic shock Cardiac resuscitation Hemostasis (topical use) Prolong local anesthetic effect (local use) Open-angle glaucoma Nasal congestion. Can be used for acute asthmatic attack and anaphylaxis, high doses of locally applied epinephrine cause vasoconstriction which prolong the action of local anesthetics

 

CI:

 

Therapeutic Consideration:

Term
Phenoxybenzamine
Definition

 

 

Mech: Nonselective irreversible alpha adrenergic antagonist

Causing vasodilation, decreased BP, decreased peripheral resistance

 

Clinical Application:Pheochromocytoma-associated hypertension and sweating

 

Common and Serious RXNS:Postural hypotension, tachycardia, palpitations, xerostomia, sedation, miosis, absence of ejaculation

 

 

CI:Severe hypotension; coronary artery disease (phenotolamine

 

 Therapeutic Consideration:blocks irreversibly; used in preoperative management of pheochromocytoma hypertension

Term
Propranolol
Definition

 

 

Mech:Nonselective

Beta adrenergic antagonist

Block
beta adrenergic receptors

 

Clinical Application:Hypertension,

angina, heart failure, pheochromocytoma, glaucoma (timolol ocular formulation)

 

Common and Serious RXNS:Bronchospasm,

atrioventricular block bradyarrhythmia; Sedation,
decreased libido, mask symptoms of hypoglycemia, depression, dyspnea, wheezing

 

CI: Bronchial asthma or COPD; cardiogenic shock; uncompensated cardiac failure; second and

third degree AV block; severe sinus bradycardia

 

Therapeutic Consideration:Block beta 1 and 2 receptors equally

EXTREMELY LIPOPHILIC
CNS concentration is sufficiently HIGH that sedation and decreased libido may result

Term
Reserpine
Definition

 

 

Mech:Inhibitors of catecholamine

storage
irreversible VMAT inhibitor

 

Clinical Application:hypertension

 

Common and Serious RXNS:cardiac arrhythmia, gastrointestinal hemorrhage, thrombocytopenia, dream anxiety disorder, impotence, psychotic depression, dizziness, nasal congestion

 

CI:active gastrointestinal disease;

depression; electroshock therapy; renal therapy

 

Therapeutic Consideration:irreversibly damages VMAT,

resulting in vesicles that lose the ability to concentrate and store NE and DA;
rarely used as a therapeutic agent due to its irreversible action and its
association with psychotic depression

Term
Tranylcypromine
Definition

 

 

Mech:Nonselective MAOI – increasing catecholamine

levels by blocking catecholamine degradation

 

Clinical Application: Depression

 


Common and Serious RXNS:


Systemic tyramine toxicity from eating
foods that contain tyramine (uncontrolled catecholamine release can induce a
hypertensive crisis characterized by headache, tachycardia, nausea, cardiac
arrhythmia, and stroke); fever associated with increased muscle tone, leucopenia,
hepatic failure, drug induced lupus, worsening depression

Dizziness, somnolence,
orthostatic hypotension, weight gain, increased liver aminotransferase level,
orgasm disorder

 

 

CI:Concomitant use of

sympathomeimetic drugs; concomitant bupropion, buspirone, guanethidine, other
MAOIs, serotonergic drugs; concomitant methyldopa, L-dopa, L-tryptophan,
L-tyrosine, phenylalanine; concomitant CNS depressants, narcotics,
dextromethorphan; concomitant, excessive coffee or chocolate intake;
concomitant foods with high tyramine content (cheese, beer, wine, pickled
herring, yogurt, liver, yeast extract); liver disease; pheochromocytoma, heart
failure, general anesthesia, local anesthesia with vasoconstrictors

 

Therapeutic Consideration:Due to the extensive effects of

MAOIs on P450 enzymes; MAOIs can cause extensive drug-drug interactions;
extreme caution must be used when prescribing medications to patients
concurrently taking a MAOI; irreversible nonselective MAOI; most toxic effect
is systemic tyramine toxicity; the older, nonselective MAOIs are no longer
considered first-line therapy for depression because of their significant
potential for tyramine toxicity; can precipitate manic or hypomanic episodes in
some bipolar patients

Term
Imipramine
Definition

 

 

Mech:Inhibitor of catecholamine

reuptake

Inhibit norepinephrine transporter
(NET) mediated reuptake of catecholamines, potentiating catecholamine action

 

Clinical Application:Depression, pain syndromes such as migraine headaches, chronic fatigue syndrome, and other somatic

pain disorders; nocturnal enuresis

 

Common and Serious RXNS:


Heart block, cardiac arrhythmia, orthostatic hypotension, myocardial infarction, agranulocytosis, jaundice, seizure,
worsening depression with suicidal thoughts; Bloating, constipation,
xerostomia, dizziness, somnolence, blurred vision, urinary retention

 

CI:


Concomitant use of monoamine oxidase inhibitors;
cardiac conduction system defects; use in patients during acute recovery after a myocardial infarction

 

Therapeutic Consideration:Affect cardiac sodium channels in quinidine-like

manner leading to potentially lethal conduction delays; an ECG should be done to rule out conduction system disease prior to starting TCAs; concurrent use of other agents that affect the
cardiac conduction system requires careful monitoring; pressor response to IV epinephrine
may be markedly enhanced; orthostatic hypotension is a significant adverse effect for elderly patients; can precipitate mania in patients with bipolar
disorder

Term
Prazosin
Definition

 

 

Mech:selective antagonists of α1-receptors in arterioles and veins

 

Clinical Application:Hypertension Benign prostatic hyperplasia

 

Common and Serious RXNS:Pancreatitis, hepatotoxicity, systemic lupus erythematosus Marked first-dose postural hypotension, palpitations, dyspepsia, dizziness, sedation, increased urinary frequency, nasal congestion

 

CI:Hypersensitivity

 

Therapeutic Consideration:Due to potential severe postural hypotension, first dose is generally prescribed in small quantities at bedtime (to ensure that the patient remains supine); Shorter half life than Terazosin/doxazosin; TCAs may increase rist of posural hypotension.

Term
Esmolol
Definition

 

 

 Mech:β1-selective adrenergic antagonist.

 

Clinical Application:Hypertension, angina, heart failure, thyroid storm.

 

 Common and Serious RXNS:Bronchospasm, atrioventricular block, bradyarrhythmia,sedation, decreased libido, mask symptoms of hypoglycemia, depression, dyspnea, wheezing, not as much bronchospasms as propranolol

 

CI:Bronchial, asthma, or chronic obstructive pulmonary disease. Cardiogenic shock, uncompensated cardiac failure. Second- and third-degree AV block, severe sinus bradycardia.

 

Therapeutic Consideration:Esmolol has an extremely short half-life (3–4 min), and because of this, is used for emergency β-blockade, as in thyroid storm.

Term
Celiprolol
Definition

 

 

 Mech:β1-Selective antagonist and β2-selective agonist

 

Clinical Application:Hypertension, angina, heart failure.

 

Common and Serious RXNS:Bronchospasm, atrioventricular block, bradyarrhythmia,sedation, decreased libido, mask symptoms of hypoglycemia, depression, dyspnea, wheezing, not as much bronchospasms as propranolol.

 

CI:Bronchial, asthma, or chronic obstructive pulmonary disease. Cardiogenic shock, uncompensated cardiac failure. Second- and third-degree AV block, severe sinus bradycardia.

 

Therapeutic Consideration:

not approved in US

Term
Acebutolol
Definition

 

 

Mech:β1-selective partial agonist.

 

Clinical Application:Hypertension, angina.

 

Common and Serious RXNS:Bronchospasm, atrioventricular block, bradyarrhythmia,sedation, decreased libido, mask symptoms of hypoglycemia, depression, dyspnea, wheezing.

 

CI:Bronchial, asthma, or chronic obstructive pulmonary disease. Cardiogenic shock, uncompensated cardiac failure. Second- and third-degree AV block, severe sinus bradycardia.



Therapeutic Consideration:Acebutolol is a partial agonist at β1-adrenoceptors but has no effect at β2-receptors.

Term
Pindolol
Definition

 

Mech:Partial agonist at β1- and β2-receptors (non-selective). Blocks the action of endogenous norepinephrine at β1-receptors. As a partial agonist causes partial stimulation of β1-receptors, which leads to overall smaller decreases in resting heart rate and blood pressure compared to those caused by pure β-antagonists.

 

Clinical Application: Hypertension, angina.

 

Common and Serious RXNS:Bronchospasm, atrioventricular block, bradyarrhythmia,sedation, decreased libido, mask symptoms of hypoglycemia, depression, dyspnea, wheezing, not as much bronchospasms as propranolol.

 

CI:Bronchial, asthma, or chronic obstructive pulmonary disease. Cardiogenic shock, uncompensated cardiac failure. Second- and third-degree AV block, severe sinus bradycardia.

 

Therapeutic Consideration:Pindolol is a partial agonist at β1- and β2- receptors; it is preferred in hypertensive patients who have bradycardia or decreased cardiac reserve.

Term
Carvedilol
Definition

 

 

Mech:Nonselective β- and α1-Antagonist. Cause a decrease in blood pressure. The α1-receptor blockade results in vasodilation. The β1-blockade prevents a reflex sympathetic increase in heart rate.

 

Clinical Application:Hypertension, angina.

 

Common and Serious RXNS:Bronchospasm, atrioventricular block, bradyarrhythmia,sedation, decreased libido, mask symptoms of hypoglycemia, depression, dyspnea, wheezing.

 

CI:Bronchial, asthma, or chronic obstructive pulmonary disease. Cardiogenic shock, uncompensated cardiac failure. Second- and third-degree AV block, severe sinus bradycardia.

 

Therapeutic Consideration:Carvedilol block α1-, β1-, and β2-receptors.Intermediate half-life.

Term
Timolol
Definition

 

 

Mech:Non-selective β-antagonist. Mech: Block β-adrenergic receptors. *Short half-life*

 

Clinical Application:Hypertension; Angina; Heart failure; Pheochromocytoma; Glaucoma (timolol ocular formulation)

 

Common and Serious RXNS:Serious: Bronchospasm, atrioventricular block, bradyarrhythmia; Common: Sedation, decreased libido, mask symptoms of hypoglycemia, depression, dyspnea, wheezing

 

CI:Bronchial asthma or chronic obstructive pulmonary disease; Cardiogenic shock; Uncompensated cardiac failure; Second- and third-degree AV block; Severe sinus bradycardia

 

Therapeutic Consideration:Propranolol, nadolol, and timolol block β1- and β2-receptors equally; An ocular formulation of timolol is used in the treatment of glaucoma.

Term
Nadolol
Definition

 

 

 Mech:Non-selective β-antagonist. Mech: Block β-adrenergic receptors. *Long half-life*

 

Clinical Application:Hypertension; Angina; Heart failure; Pheochromocytoma [F/Internet: Pheochromocytoma is a rare type of tumor that usually develops in the inner portion (medulla) of the adrenal glands. The tumor causes excess release of Epi & NE, hormones causing intermittent or sustained periods of high blood pressure.]

 

Common and Serious RXNS:Serious: Bronchospasm, atrioventricular block, bradyarrhythmia; Common: Sedation, decreased libido, mask symptoms of hypoglycemia, depression, dyspnea, wheezing

 

CI:Bronchial asthma or chronic obstructive pulmonary disease; Cardiogenic shock; Uncompensated cardiac failure; Second- and third-degree AV block; Severe sinus bradycardia

 

Therapeutic Consideration:Propranolol, nadolol, and timolol block β1- and β2-receptors equally

Term
Yohimbine
Definition

 

 

Mech:Selective blockade of α2-autoreceptors (α2 antagonist)

Selectivity: α2 >> α1. Mech: Block endogenous catecholamines from binding to α1- and α2-adrenoceptors, causing vasodilation, decreased blood pressure, and decreased peripheral resistance.

 

Clinical Application:Organic and psychogenic impotence (Used in the past to treat erectile dysfunction, but Phosphodiesterase type 5 inhibitors have widely replaced its use)

 

Common and Serious RXNS:Common: Bronchospasm, nervousness, tremor, anxiety, agitation, increased blood pressure, antidiuresis

 

CI:Chronic inflammation of sexual organs or prostate gland, Concurrent use with mood altering drugs, Gastric and duodenal ulcers, Pregnancy, Psychiatric patients, and Renal and liver disease.

 

Therapeutic Consideration:Yohimbine is an α2-selective antagonist that leads to increased release of norepinephrine, which stimulates cardiac β1-receptors and peripheral vascular α1-receptors. It also leads to increased insulin release due to blockade of α2-receptors in pancreatic islets.

Term
Phentolamine
Definition

 

 

 Mech:REVERSIBLE NON-selective alpha-adrenergic ANTAGONIST. Blocks endogenous catecholamines from binding to alpha-1 and alpha-2 adrenoceptors. Causes vasodilation, decreased blood pressure and decreased peripheral resistance. Baroreceptor reflex will attempt to compensate for the fall of blood pressure which in turn increases heart rate and cardiac output.

 

Clinical Application:Used in preoperative management of pheochromocytoma associated hypertension and sweating. (According to the Mayo Clinic Pheochromocytoma is a rare, usually noncancerous (benign) tumor that develops in the core of an adrenal gland. This leads to increased production of blood pressure rising hormones.)

 

Common and Serious RXNS:Seizure. Postural hypotension, tachycardia, palpitations, xerostomia, sedation, miosis, absence of ejaculation.

 

CI:Severe hypotension. Coronary artery disease (phentolamine).

 

Therapeutic Consideration:Equal affinity to alpha 1 and alpha 2 receptors

Term
Terazosin
Definition

 

 

Mech:Alpha-adrenergic ANTAGONIST. Longer half-life than prazosin. Falls under the Prazosin class

 

Clinical Application: Hypertension. Benign prostatic hyperplasia

 

Common and Serious RXNS:Pancreatitis, hepatotoxicity, systemic lupus erythematosus. Marked first-dose postural hypotension, palpitations, dyspepsia, dizziness, sedation, increased urinary frequency, nasal congestion.

 

CI:Hypersensitivity to prazosin or doxazosin.

 

 Therapeutic Consideration:Prazosin, terazosin, and doxazosin are nonsubtype selective antagonists of α1-receptors in arterioles and veins. Reflex tachycardia does not usually occur. Due to potential severe postural hypotension, first dose is generally prescribed in small quantities at bedtime (to ensure that the patient remains supine). Terazosin has longer half-life than Prazosin. Tricylic antidepressants may increase the risk of postural hypotension.

Term
Doxazosin
Definition

 

 

Mech:α1 >>>> α2 adrenergic antagonists; in Prazosin class, but (like Terazosin) has a longer half-life allowing less frequent dosing. Mech: Block endogenous catecholamines from binding to α1- and α2-adrenoceptors, causing vasodilation, decreased blood pressure, and decreased peripheral resistance.

 

Clinical Application: Hypertension; Benign prostatic hyperplasia

 

Common  Adverse Reactions:Serious: Pancreatitis, hepatotoxicity, systemic lupus erythematosus; Common: Marked first-dose postural hypotension, palpitations, dyspepsia, dizziness, sedation, increased urinary frequency, nasal congestion 

 

CI: Hypersensitivity to prazosin, terazosin, or doxazosin

 

Therapeutic Reactions: Doxazosin (also Prazosin & terazosin) are nonsubtype selective antagonists of α1-receptors in arterioles and veins; Reflex tachycardia does not usually occur; Due to potential severe postural hypotension, first dose is generally prescribed in small quantities at bedtime (to ensure that the patient remains supine- Supine = Lying face upward.); Terazosin and doxazosin have a longer half-life than prazosin. Tricylic antidepressants may increase the risk of postural hypotension

 

Term
Tamsulosin
Definition

 


Mech: Specific antagonist at α1A-receptors (Little effect at α1B- or α1C-subtypes); Mech: Block endogenous catecholamines from binding to α1- and α2-adrenoceptors, causing vasodilation, decreased blood pressure, and decreased peripheral resistance.


Clinical Application:Benign prostatic hyperplasia; May decrease the incidence of orthostatic hypotension (when BP falls suddenly when standing up or stretching).



Common Reactions: Same as prazosin (S: Pancreatitis, hepatotoxicity, systemic lupus erythematosus; C: Marked first-dose postural hypotension, palpitations, dyspepsia, dizziness, sedation, increased urinary frequency, nasal congestion), except less postural hypotension.

 

CI:Hypersensitivity to tamsulosin

 

Therapeutic Applications: Tamsulosin is a subtype-selective α1A-receptor antagonist that has more specificity toward smooth muscle in genitourinary tract; thus, tamsulosin has lower incidence of orthostatic hypotension

Term
Dopamine
Definition

 


Mech: Beta adrenergic agonist


CA:In distributive or

cardiogenic shock, use as
adjunct to increase cardiac
output, blood pressure, and
urine flow
Short-term treatment of
severe, refractory, chronic
heart failure



Side Effects: Frequently used in the emergency treatment of distributive shock. Blood pressure support in acute hypotensive states (shock) Limit GI bleeding via intraperitoneal or nasogastric administration


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