Term
| List of Direct Acting Muscarinic Agonists |
|
Definition
Acetycholine (Miochol-E)
Carbachol(Isopto Carbachol)
Methacholine
Bethanechol(Urecholine)
Pilocarpine (Salagen, Isopto Carpine)
muscarine |
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Term
| Actions of Direct Muscarinic Agonists |
|
Definition
Inc. GI motility and secretion
Inc. HR
Inc. BP (due) to dec. CO and direct vasodiation
contraction of bladder and relaxation of urinary sphincters
miosis and decreased intraocular pressure
stimulation of secretions |
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Term
| Adverse effects of Direct acting muscarinic agonists |
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Definition
| Due to unwanted or excessive muscarinic stimulation (overexpression of any normal muscarinic-mediated action) |
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Term
| Major therapeutic uses of direct acting muscarinic agonists |
|
Definition
promote GI motility (bethanecol)
Treatment of Urinary retention (bethanecol)
treatment of glaucoma(pilocarpine, acetylcholine, carbachol)
treatment of salivary gland dysfunction (pilocarpine)
pulmonary function testing in asthma (methacholine) |
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|
Term
| Contraindications or cautions for Direct acting muscarinic agonists |
|
Definition
asthma
bradycardia, hypotension, vasomotor instability, or coronary artery disease
peptic ulcer disease
hyperthyroidism
weakend smooth muscle of the bladder or GI tract (post surgery or intestinal anastomosis)
urinary or intestinal obstruction
NEVER TO BE GIVEN IV OR IM, only sub-q, oral or topicallyy (eye) |
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Term
| Treatment of Glaucoma, rapidly hydrolyzed to pseudocholinesterase in the plasma |
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Definition
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|
Term
Analog of acetylcholine, resistant to hydrolysis by cholinesterases
can stimulate both muscarinic and nicotinic receptors
used topically on opthalmology for treatment of glaucoma |
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Definition
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|
Term
analog of acetylcholine
stimulates muscarinic but little effect on nicotinic
used in pulmonary function testing in asthma |
|
Definition
|
|
Term
Analog of acetylcholine that is resistant to rapid hydrolysis
little effect at nicotinic
stimulate GI motility and treat urinary retention |
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Definition
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Term
| muscarinic agonist used in treatment of glaucoma and xerostomia due to poor salivary secretion |
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Definition
| pilocarpine (salagen, ocusert pilo) |
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Term
| List of reversible cholinesterase inhibitors |
|
Definition
edrophonium (tensilon)
physostigmine (eserine)
neostigmine(prostigmin)
pyridostigmine(mestinon)
rivastigmine(exelon_
donepezil* |
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Term
| muscarinic agonist used in treatment of glaucoma and xerostomia due to poor salivary secretion |
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Definition
| pilocarpine (salagen, ocusert pilo) |
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Term
| List of reversible cholinesterase inhibitors |
|
Definition
edrophonium(tensilon_
physostigmine(eserine_
neostigmine(prostigmin)
pyridostigmine(mestinon)
rivastigmine(exelon)
donepezil (aricept)
carbamate insecticides(carbaryl) |
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Term
| list of irreversible or slowly reversible cholinesterase inhibitors |
|
Definition
DFP/diisopropylfurophosphate/isoflurophate and echothiophate
organophosphate insecticides (parathion, malathion)
nerve gases (sarin) |
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Term
| Cholinesterase reactivator (name) |
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Definition
| pralidoxime/2-PAM (protopam) |
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|
Term
| cholinesterase inhibitor action |
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Definition
| prevent breakdown of acetylcholine in the synapse, leads to elevated synaptic levels of acetylcholine at Parasym. end organs, autonomic ganglia and neuromuscular junction. |
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Term
| Actions of cholinesterase inhibitors |
|
Definition
inc. GI motility and secretion
contraction of bladder, relaxation of urinary sphincter
bradycardia and hypotension
increased secretion
decreased intraocular pressure
stimulation of skeletal muscle
bronchoconstriction |
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|
Term
| toxic effects of cholinesterase inhibitors |
|
Definition
SLUDGE-salivation, lacrimation, urination, defecation, GI distress, emesis)
skeletal muscle fasciculations followed by paralysis
bradcardia, hypotension, shock
severe miosis
CNS stimulation and seizures followed by coma
demyelination of axons (chronic exposure) |
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|
Term
| treatment of acute cholinesterase inhibitor poisoning |
|
Definition
high doses of atropine (2-4 mg IV initially) followed by 2 mg IM every 10 mins till symptoms disappear
pralidoxime to reactivate enzyme (organo-phosphates only)
supportative...diazepam for seizures |
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|
Term
| Therapeutic uses of cholinesterase inhibitors |
|
Definition
Diagnosis(edrophonium) and treatment(neostigmine, pyridostigmine) of myasthenia gravis....Tensilon test uses edrophonium to test for improvement of muscle strength
Treat glaucoma(echothiophate)
Treatment of Alzheimers (rivastigmine, donepezil
treatment of poisoning by atropine or other antimuscarinics(physostigmine)
reversal of neuromuscular blockade(neostigmine or pyridostigmine)
treatment of atony of the bladder or GI tract
"pre-exposure antidotal enhancement" - pyridostigmine |
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Term
| Contraindications for cholinesterase inhibitors |
|
Definition
asthma
bradycardia, hypotension, coronary artery disease
peptic ulcer disease
urinary or intestinal obstruction |
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|
Term
Edrophonium (tensilon)
neostigmine (prostigmin)
pyridostigmine (mestinon) |
|
Definition
reversible cholinesterase inhibitors
quaternary ammonium compounds that dont enter the CNS
edrophonium is short acting (<10 mins) and is used in diagnosing myasthenia gravis
neostigmine and pyridostigmine are longer acting and are used in the treatment of myasthenia gravis |
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Term
| physostigmine/eserine (antilirium) |
|
Definition
reversible cholinesterase inhibitor
nonquaternary so it CAN get into the CNS
used to treat atropine poisoning or other antimuscarinics |
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Term
| organophosphate insecticides (parathion, malathinon) |
|
Definition
must be oxidized to active metabolites (occurs faster in insects than humans)
treat poisoning with atropine or pralidoxime and also symptomatic |
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Term
| Carbamate insecticides (carbaryl) |
|
Definition
not absorbed through the skin as well as organophosphate insecticides
treat poisoning with atropine
pralidozime is NOT useful for treating carbamate insecticide poisoning |
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Term
| DFP/isoflurophate and nerve gases(sarin) |
|
Definition
potent and toxic, irreversible cholinesterase inhibitor
treat poisoning with atropine and pralidoxime
DFP/isoflurophate has been used for glaucoma |
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Term
| Pralidoxime/2-PAM (protopam) |
|
Definition
chilinesterase reactivator, chemically binds phosphate that is inhibiting enzyme
for organophosphate poisoning, must be used withing 2 hours
does not work with carbamate insecticides |
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Term
| Sildenafil(Viagra), Vardenafil (levitra), tadalafil (cialis) |
|
Definition
MoA:inhibition of cyclic GMP PDE-5, which breaks down cGMP
Side effects: general vasodilation, can result in hypotension with reflex increase in HR (may cause problems in men with previous CV disease)
may cause troubles with blue/green discrimination
may cause auditory disturbances
Oral use, metabolized by CYP3A4(adjust doses for patients with renal or hepatic disease)
drug interactions: drugs metabolized by CYP3A4(erythromycin, ketaconazole, cimetidine), vasodilators (nitrates, calcium channel blockers, alpha 1 blockers), sympathomimetics |
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|
Term
| Onset of Action and duration for Sildenafil(Viagra), Vardenafil (levitra), tadalafil (cialis) |
|
Definition
Sildenafil(Viagra) ~30 mins....4 hours
Vardenafil (levitra)~30 mins...4 hours
tadalafil (cialis) ~45 mins...36 hours |
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Term
| List of Anticholinergic Drugs |
|
Definition
Atropine (hyoscyamine)
Scopolamine(hyoscine)
dicyclomine(bentyl)
propantheline
glycopyrrolate(robinul)
ipratropium(atrovent)
tiatropium(spiriva)
benztropine(cogentin)
trihexyphenidyl(artane)
tolterodine(detrol)
oxybutynin(ditropan)
solifenacin(vesicare)
tropicamide(mydriacyl) |
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Term
| Pharmacologic Effects of anticholingergic drugs |
|
Definition
act as competitive antagonists at muscarinic receptors:
drying of secretions
decrease tone and motility of GI
relaxation of bladder and urine retnetion
bronchodilation
mydriasis with cycloplegia and increased intraocular pressure
increased HR
CNA-sedation and amnesia at low doses, excitation and seizures and toxic doses |
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|
Term
| Side effects of anticholinergic drugs |
|
Definition
dry mouth
dry,hot skin
constipation, urinary retention
visual disturbances, blurred vision, photophobia
CNS effects- sedation, confusion, amnesia(esp in elderly) |
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|
Term
| contraindications and precautions for anticholinergic drugs |
|
Definition
glaucoma
prostatic hypertrophy
CV instability
severe ulcerative colitis |
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|
Term
| Symptoms and treatment of Acute poisoning with antimuscarinic(anticholinergic) agents |
|
Definition
Symptoms: dry, hot skin and hyperthermia, severe mydriasis, blurring of vision, photophobia, CNS stimulation-agitation, hallucinations, seizures progressing to coma and death, cessation of GI motility (no bowel sounds), weak rapid pulse, tachycardia and arrhythmias
Treatment: administration of physostigmine or other cholinesterase inhibitors, benzodiazepenes for treatment of seizures, ice baths to reduce hyperthermia, dark quiet environment to keep relaxed and prevent photophobia |
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|
Term
| Atropine and Homatropine effects |
|
Definition
Naturally occurring belladonna alkaloid found in nightshade plant
Effects:
Heart- tachycardia, slight increase in CO (initially may have a transient bradycardia)
blood vessels-can reverse the hypotensive actions of acetylcholine or other muscarinic agonists
Eye- 3 clinically relevant effects...mydriasis,cycloplegia, increased intraocular pressur...if patient has glaucoma, pressure can reach catastrophic levels
GI- inhibitory effects on motility and tone
Urinary Tract- relaxes bladder and contracts sphincter
Sweat Glands - inhibits sweating(children-hyperthermia susceptible)
Salivary Glands- "dry mouth"
Respiratory tract- bronchodilation and drying of secretions throughout RT
CNS- low doses sedation, high doses stimulant |
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Term
| atropine and homatropine therapeutic uses |
|
Definition
preop medication to reduce secretions and block vagal reflexes on the heart
cardiac stimulant following some types of MI(ie increase in vagal tone)
antidote for poisoning with cholinesterase inhibitors or muscarinic agonists
pulmonary medicine to dry respiratory secretions
mydriatic and cycloplegic agent in opthalmalogy
antispasmodic for treatment of GI disorders such as IBS and biliary colic |
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|
Term
| Scopolomine(hyoscine) and methscopolamine |
|
Definition
antimuscarinic, Natural product found in plant Hyoscyamus niger(Henbane), quaternary analog(doesnt cross BBB)
similar to atropine in pharmacologic effects except it has more of a CNS depressant effect than atropine
orally and in patch form for motion sickness and vertigo |
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Term
|
Definition
nonquaternary antimuscarinic agent
widely used as antispasmodic for treatment of IBS |
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Term
| Propantheline(Pro-Banthine) |
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Definition
| antimuscarinic, used for treatment of IBS, quaternary, few CNS effects |
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|
Term
|
Definition
antimuscarinic, Quaternary, no CNS effects, preop to dry secretions and inhibit vagal reflexes
general purpose antimuscarinic |
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Term
| Ipratropium(Atrovent) and Tiatropium(Spiriva) |
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Definition
| antimuscarinic, quaternary, administered by inhalation for treatment of asthma and COPD, few systemic effects, tiatropium is newer with longer duration |
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Term
| Benztropine(cogentin) and trihexyphenidyl(artane) |
|
Definition
| centrally acting antimuscarinics used in the treatment of Parkinsons disease or drug induced parkinsonism |
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Term
| Tolterodine(detrol), oxbutynin(ditropan) and solifenacin(vesicare) |
|
Definition
| antimuscarinic agents approved for use in treatment of urinary incontinence due to over active bladder |
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Term
|
Definition
| antimuscarinic agent widely used to dilate the pupil for ophthalmologic examination |
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Term
| competitive neuromuscular blocking drugs |
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Definition
| main one is Pancuronium(Pavulon), acts as a competitive Ach antagonist and neuromuscular junction to produce muscle relaxation |
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Term
| Depolarizing Agents of the Neuromuscular Blocking Drugs |
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Definition
| Succinylcholine(Anectine) is the main one, initially stimulates receptors to cause weak contractions followed by relaxation and paralysis |
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Term
| Mixed or nonselective Direct acting Sympathomimetics (adrenergic receptor agonists) |
|
Definition
Epinephrine(adrenalin, Epipen, primatene mist)
Norepinephrine(Levophed)
Isoproterenol(isuprel)
Dopamine(intropin) |
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|
Term
|
Definition
|
|
Term
|
Definition
Albuterol(Proventil)
Metaproterenol
pirbuterol(maxair)
salmeterol (serevent)
Terbutaline |
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|
Term
| Indirect-acting symathomimetics |
|
Definition
Cocaine
pseudoephedrine(sudafed) and ephedrine
amphetamine and methamphetamine
methylphenidate(ritalin) |
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|
Term
| Rate limiting step of NE production |
|
Definition
| Tyrosine to DOPA via tyrosine hydroxylase |
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Term
| autonomic receptors and effects for the eye |
|
Definition
Symp - mydriasis(a1), increase ciliary aqueous production (B2)
Para - miosis, contraction of ciliary muscle |
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Term
| autonomic receptors and effects for the heart |
|
Definition
Symp- SA node increased rate, ventricle increased contractility, SA and AV nodes increased automaticity and conduction velocity (all B1 and B2)
Para- decreased rate, contractility, automaticity, conduction velocity (all muscarinic) |
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Term
| autonomic receptors and effects for the blood vessels of mucosa, skin, and splanchnic beds |
|
Definition
symp-constriction(a1 and a2)
para-dilation |
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|
Term
| autonomic receptors and effects for the blood vessels of skeletal muscle |
|
Definition
symp-constriction(a1), dilation (B2)
para- dilation |
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|
Term
| autonomic receptors and effects for the lungs |
|
Definition
symp -relaxation (B2)
para-constriction |
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|
Term
| autonomic receptors and effects for the GI tract |
|
Definition
symp-relaxation, decreased motility (all 4 types)
para- increased motility, increased spasms |
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Term
| autonomic receptors and effects for the bladder |
|
Definition
symp-relaxation of wall (B2), contraction of sphincter and prostate(a1)
para- constriction of wall, relaxation of sphincter |
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Term
| autonomic receptors and effects for the kidney (JG cells) |
|
Definition
| symp- increased renin secretion(B1) |
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Term
| autonomic receptors and effects for the uterus |
|
Definition
| symp - contraction (a1), relaxation (B2) |
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Term
| autonomic receptors and effects for the male sex organs |
|
Definition
symp-ejaculation(a1)
para- erection |
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|
Term
| autonomic receptors and effects for the liver and fat cells |
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Definition
| symp-increase glucose output (B2), increase fatty acid output (B1) |
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Term
| autonomic receptors and effects for the skin |
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Definition
| symp- contraction of pilomotor muscle (a1), secretion of sweat glands (muscarinic) |
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Term
|
Definition
mix or nonselective symp agonist
stimulates all a and B nearly alike
low IV rates of E will decrease diastolic, and increase systolic, pp, and hr(a2 and B2), higher rates cause increase in diastolic as well
used in circulatory shock (B2 bronchial, vascular alpha, cardiac ventricular B2)
bronchodilation in asthma(B2)
treat cardiac arrest (cardiac B, vascular a)
treatment of bradycardia due to AV block(AV node B, purkinje B)
mixed with local anesthetics to prolong action at local sites of injection |
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Term
|
Definition
nonselective symp agonist
affects all adrenergic except B2 nearly alike
IV infusion increases all cardiac pressures and reflexively decreases HR (more drug means more effect)
most uses due to effects on vascular a receptors
sometimes used in shock...cardiogenic or neurogenic(involves cardiac B1 and/or vascular alpha)
support of BP during spinal anesthesia |
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Term
|
Definition
stimulates all B but not alpha receptors (nonspecific symp agonist)
IV infusion increases rate contractility automaticity and conduction velocity
used as a pharmacologic provocation to assist tilt-table tests for diagnosis of unexplained syncopes(eg vasovagal syncope) |
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|
Term
|
Definition
stimulates dopamine receptors in GI and renal arterial smooth muscle starting at low doses(increases blood blow to GI and kidney), B1 receptors at intermediate doses(cardiac effects), and a1 receptors at even higher doses(increase total peripheral vascular resistance)
some forms of shock(cardiogenic and neurogenic)...B1 or a1 for treating shock(dose dependent)
used for patients with congestive heart failure who may be refractory to other forms of therapy |
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Term
|
Definition
Selective B1 agonist
administered as a mix of two stereoisomers, one is a1 agonist, other is potent B1 agonist and a1 antagonist..net effect is fairly selective B1 stimulation
used in CHF and certain forms of shock
sometimes used to stimulate the heart during emergence from surgery |
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Term
| Albuterol, metaproterenol, pirbuterol, salmeterol, and terbutaline |
|
Definition
fairly selective B2 agonist
Bronchodilators to treat patients with COPD and asthmatics
most often inhalers, though oral and IV exist
terbutaline - manage premature labor, uterine relaxation (terbutalINE - uterINE) |
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Term
| Phenylephrine and midodrine |
|
Definition
Alpha 1 agonists
Phenylephrine: IV to maintain diastolic and mean BP during neurogenic shock or spinal anesthesia...treat hemorrhoids and nasal congestion...mydriatic...IV to treat supraventricular tachycardias
Midodrine(a prodrug) better absorbed with oral administration than phenylephrine...treats orthostatic hypotensive symptoms |
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Term
|
Definition
indirect symp. agent
inhibits NE reuptake at nerve terminals, thus keeping receptors activated. |
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|
Term
| Pseudoephedrine/ephedrine |
|
Definition
like tyramine,stimultes NE from symp nerve endings independent of AP's, but stimulate adrenergic receptors directly
treats nasal and bronchial congestion |
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Term
| Pharmacological properties of B-blockers |
|
Definition
competitive antagonists at B1 receptors
some block B2 as well
B1-cardioselective (heart has high amts of B1 receptors)
some can also be considered partial agonists of B-receptors, with the net effect of preservation of at least a small amt of B-receptor function
Some stabilize cell membranes(local anesthetic action)
lipid solubility-high means entry to brain and metabolism by liver...esmolol is an exception(inactivated by esterases) |
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Term
| Actions and uses of B1-receptor Blockers |
|
Definition
B1 in heart-lower HR, contractility, automaticity and conduction velocity (antianginal use due to HR and contractility's effect of decreases O2 deficit after MI
prevent post MI arrythmias(decreased automaticity), prevent abnomrmal supraventricular tachycardias and arrythmias(conduction velocity)
protects the heart during surgical removal of a phheocromocytoma or from a thyroid storm in hyperthyroidism |
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Term
| Actions of B2-receptor blockers |
|
Definition
may have similar effects as B1 on heart, but not proven
applied topically to treat glaucoma (reduces intraocular pressure)...drug of choice tends to be timolol |
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Term
| actions of B-blocks as partial agonists (ISA) |
|
Definition
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|
Term
| uses of B-blockers in terms of membrane stabilization, as well as lipid solubility |
|
Definition
Membrane Stabilization - contribute to anytiarrhythmic action of propanolol
Lipid solubility- higher solubility can allow antihypertensive effects on CNS...high solubility requires a good liver for metabolism, and low solubility requires healthy kidneys...Esmolol-short duration(10 mins), rapid inactivation by plasma and blood cell esterases, can be used for acute treatment of supraventricular arrhythmia, perioperative hypertension, and MI |
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Term
| Side effects of B-blockers |
|
Definition
with relation to:
B1 - excessive depression of myocardial B1 receptor function, decreased CO, aggravate Raynauds and intermittent claudication, exercise intolerance, hides marked tachycardia that normally occurs before severe hypoglycemic rxn to insulin
B2- Bronchoconstriction, intermittent claudication and exercise intolerance, delayed revocery from insulin-induced hypoglycemic episodes.
partial agonist- less severe overall in relation to others.
membrane stabilization - undesirable local anesthetic effects of eye
other - aggravate insulin-resistant states in hypertensive or type 2 diabetic patients, aggravate or induce abnormal blood lipid profiles |
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Term
| Labetalol - type of drug, action |
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Definition
| combination nonselective B-blocker and selective a1-blocker used to treat moderate to severe primary hypertension (orally) and for emergency treatment of hypertensive crisis(IV) |
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Term
| names of combination drugs related to beta blockers (four of them) |
|
Definition
Labetalol(NS B-blocker/a1-blocker)
nebivolol (B1-blocker/endothelium dependent vasodilator)
carvedilol (B-blocker/a-blocker/antioxidant)
sotalol (b-blocker/k-channel blocker) |
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Term
| LIST the B-blockers, and comment on their selectivity, partial agonist activity, membrane stabilizaing ability, and lipid solubility |
|
Definition
***CHART IN LECTURE 16, PAGE 1***
Acebutolol(sectral)-B1, partial agonist, membrane stabilizing, Low(?) solubility
Atenolol(tenormin) - B1, low solubility
Esmolol(Brevibloc)- B1, low solubility (FAST acting)
Metoprolol(Lopressor, Toprol-XL) - B1, maybe membrane stabilizing, medium solubility
Nadolol(Corgard) - B1 + B2, low solubility
Pindolol - B1 + B2, partial agonist, membrane stabilizing(?), medium solubility
Propanolol(inderal-LA)- B1 + B2, membrane stabilizing, HIGH solubility
Timolol(timoptic) - B1 + B2, medium solubility(?) |
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Term
|
Definition
Non-selective - pheNoxybenzamine(Dibenzyline)
pheNtolamine (generic, OraVerse)
Selective a1-blockers-
Prezosin(minipress)
Terazosin(Hytrin)
Doxazosin(Cardura)
Tamsulosin(Flomax)
Alfuzosin(Uroxatral)
Silodosin(Rapaflo) |
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|
Term
|
Definition
inhibition of peripheral a-adrenergic receptors most important
non-competitive inhibition (phenoxybenzamine)- irreversible
competitive inhibition (the rest of a-blockers)
decrease BP through decreasing peripheral arterial resistance (a1 receptors cause vasoconstriction) |
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|
Term
| Side effects of a-blockers |
|
Definition
| related to too much loss of receptor action...can cause nasal congestion, difficult in ejaculation, reflex tachycardia, systemic fluid retention, and orthostatic hypotensive symptoms |
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|
Term
| Phenoxybenzamine action and side effects |
|
Definition
long active a-blocker, non selective
mainly used to prevent severe catecholamine-induced hypertensive episodes that occur in pheochromocytoma pateints (pre-operation)
better than selective blockers for this action because it also blocks extrasynaptically located a2 receptors
may inhibit histamine, serotonin and ACh receptors
miosis, sedation, drowsiness, comiting and lethargy(enters CNS)
Shock and circulatory failure |
|
|
Term
| Phentolamine action and side effects |
|
Definition
Short acting a-blocking, competitive to a1 and a2
Used in diagnosis of pheochromocytoma
reverses excess acute systemic vasoconstriction caused by NE overdose (or other a-agonists)
used to prevent local dermal tissue necrosis in cases were a-agonists were accidentally injected into muscle instead of venous lumen
can cause nausea vomiting and diarrhea
causes increased GI motility, which is bad for ulcers
may stimulate or block various non-adrenergic receptors |
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|
Term
| Prazosin action and side effects |
|
Definition
selective a1 blocker
treatment of mild to moderate primary hypertension
relax smooth muscle of bladder neck and prostatic urethra, relieving urinary problems associated with benign prostatic hyperplasia
orthostatic hypotension with syncope that only occurs on first day of treatment (first dose phenomenon) |
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|
Term
|
Definition
| newer a1 blocker, almost identical to prazosin, but longer half life so can be used for more chronic treatment |
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Term
|
Definition
| blocks subtype A of a1 receptors...treats Benign prostatic hyperplasia more specifically because those subtypes are found more prominently in the neck of the bladder and the prostate |
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|
Term
|
Definition
| a1 blocker, used to treat BPH, but (believed to be) through accumulation of drug in prostatic tissue, not due to subtype selectivity |
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Term
| List of sympathetic neuronal blockers |
|
Definition
Peripherally acting - Reserpine, Guanethidine(Ismelin)
Centrally acting- Methyldopa, Clonidine(Catapres), Guanabenz(Wytensin), Guanfacine(Tenex, Intuniv) |
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Term
|
Definition
Decreases uptake of intraneuronal DA and NE into storage vesicles, depleting stores. reduces BP by decreasing CO and peripheral arterial resistance
Side effects include sedation and mental depression due to transmitter depleting CNS nerve endings
postural hypotension, bradycardia, and fluid retention (due to periph arterial actions)
Irreversible and long-lasting even after treatment stops |
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|
Term
|
Definition
sympathetic blocker
Blocks uptake of DA and NE in storage vesicles
directly blocks NE release from nerve endings...leads to same peripheral BP effects as reserpine, not used to treat hypertension in US anymore
side effects like reserpine, but does not cause CNS side effects
interacts with tricyclic antidepressants, interfering with or antagonizing effects of guanethidine |
|
|
Term
| Alpha-methyldopa, methyldopa |
|
Definition
a2 agonist acting in central vasomotor centers, dampening the outflow of sympathetic nerve activity
Renal renin release decreases, HR and CO may decrease, arterial periph resistance decreases (main therapeutic use is treating hypertension during pregnancy)
Side effects - preipheral fluid retention, centrally mediated dry-mouth and sedation
methyldopa can cause autoimmune disorders not seen with other drugs
very rarely hemolytic anemia and/or abnormal liver function tests |
|
|
Term
|
Definition
simlar to methyldopa, though not a prodrug
dosage is smaller than methyldopa and can be absorbed through the skin (Patch form)
smoother BP control with less side effects, though may have skin rxns where patch is applied
rebound hypertension if drug stopped abruptly
Also used for: migraine, ADHD, menopausal hot flashes, PTSD
Nicotine, alcohol, and morphine withdrawal
direct injection into spinal cord may have analgesic like action |
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|
Term
|
Definition
Both similar to clonidine in terms of action
Guanabenz can also lower total serum cholesterol and causes less reactive fluid retention
Guanfacine causes slightly less sedation and less propensity to withdrawal rebound. "Intuniv" for ADHD |
|
|
Term
| Nicotine(generalities and action sites) |
|
Definition
Ganglionic stimulant at low doses(normal depolarization), but a depressant at high doses(persistent depolarization and subsequent desensitization)
action at CNS, action at CV and GI(autonomic neuronal subtype), action at skeletal muscle (muscular subtype) |
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Term
| Nicotine (details on each action site) |
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Definition
CNS-addictive effects? initial effect is stimulation (increased respiration), can cause vomiting...depression at higher doses
CVS: complex, at low doses, stimulate autonomic ganglia to produce largely adrenergic predominance such as increased peripheral vasoconstriction with acute hypertension...at higher doses may also cause a fall in BP most likely due to reversal of ganglionic stimulating action to one of a ganglionic blocking action
GI- increased motility at low doses, decreased at high doses |
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Term
| Nicotine ( Absorption, excretion, toxicity, therapuetic uses) |
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Definition
rapid acting, absorbed from all routes, metabolized in liver and excreted by kidney
passes placental and blood brain barriers
toxicity...treatment of toxicity is symptom directed...excessive stimulation could be controlled by atropine, if levels get too high and block ganglionic activity, then adrenergic agonist may become necessary
nicotine gums patches etc used to treat addiction |
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Term
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Definition
discontinued ganglionic blocking agent,used to treat very severe hypertension, tourettes, and nicotine addiction, blocked neuronal nicotinic receptors, does not affect post ganglionic autonomic nerve terminals, does not affect muscular subtypes
Several adverse rxns- postural hypotension (interference with compensatory baroreflexes), dry mouth, decreased GI and GU motility, mydriasis, cycloplegia, sedation and other CNS effects
NE used if OD (supports heart during neurogenic shock)
crosses blood brain and placental barriers, oral administration, renal excretion |
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Term
| List of Dopaminergic Agents for treatment of Parkinson's and other extrapyramidal movement disorders |
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Definition
l-DOPA
l-DOPA + carbidopa, parcopa
l-DOPA + carbidopa, entacapone
Bromocriptine
Pramipexole
Ropinirole
Amantadine |
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Term
| List of MAO-B inhibitors, COMT inhibitors, andtimuscarinics, and antihistamines, in relation to parkinsons and other movement disorders |
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Definition
MAO-B inbitors - selegiline/deprenyl
COMT inhibitor - Entacapone
Antimuscarinic - Benztropine, trihexyphenidyl
Antihistamine- Diphenhydramine |
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Term
| Drugs that raise levels of dopamine |
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Definition
| l-DOPA, selegiline/deprenyl, Entacopone |
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Term
| Drugs that stimulate post-synaptic receptors |
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Definition
| bromocryptine, pramipexole, ropinirole |
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Term
| Drugs that reduce cholingergic activity (parkinsons drugs) |
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Definition
| Benztropine, Triheriphenidyl, diphenhydramine |
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Term
| l-DOPA Pharmacokinetics and therapeutic effects |
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Definition
Absorption from GI, enters brain, metabolized to dopamine in the brain
3-4 weeks before full effect, doesnt halt progression of parkinsons, but can slow...eventually drug loses effect as disease progresses |
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Term
| Side effects and Behavioral effects of l-DOPA |
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Definition
nausea and vomiting-80%...tolerance eventually develops...divide doses to help
CV effects- postural hypotension, tachycardia, arrhythmias (although administration with carbidopa helps, be careful with patients with existing CV problems
Behavioral effects - depression, psychotic rxns, hallucinations, nightmares, euphoria, mood and personality changes, increased libido, complusiveness, more common in combo preps, lowering dose alleviates, clozapine is sometimes used for management of side effects
Choreiform movements sometimes occur |
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Term
| Variations in therapeutic responses to l-DOPA |
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Definition
| "end of dose phenomenon" "on-off" phenomenon...both refer to appearance of parkinson's symptoms |
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Term
| Miscellaneous effects of l-DOPA |
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Definition
| glaucoma, gout, hot flashes, taste and smell disturbances, elevation of liver enzymes, positve Coomb's test, blood dyscrasias, exacerbation of malignant melanoma |
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Term
| Contraindications for l-DOPA |
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Definition
| Cardiac arrhythmias, psychosis, melanoma, glaucoma, active peptic ulcer disease |
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Term
| Major Durg interactions of l-DOPA |
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Definition
Pyridoxine-enhancement of extracerebral metabolism DECREASES therapeutic effects, antipsychotics (DA antagonists) inhibit effects
MAO inhibitors can cause a hypertensive crisis
Tricyclic antidepressants- hypertensive crisis |
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Term
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Definition
inhibits DOPA decarboxylase in the periphery, more l-DOPA gets to brain!
Sinemet is the combo drug of l-DOPA and Carbidopa |
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Term
| Bromocryptine and pergolide |
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Definition
Ergot derivatives act as relatively nonspecific DA receptor agonists...less effective than l-DOPA...used in patients who do not tolerate of respond to l-DOPA
Oral administration
side effects include nausea, vomiting, postural hypotension, mental disturbances, choreiform movements, endocrine disturbances |
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Term
| Ropinirole, Pramipexole (parkinsons) |
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Definition
non-ergot dopminergic agonists (D2 and D3 receptors)
similar side effects as others
pramipexole may have antioxidant and neuroprotective effects which may slow progression of parkinsons
can be used to treat restless leg syndrome |
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Term
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Definition
antiviral originally
stimulates release of dopamine from nerve endings
less effective than l-DOPA, but more effective than anticholinergics
may potentiate the actions of l-DOPA
excreted by kidney...dosage adjustment for patients with impaired renal function |
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Term
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Definition
multiple forms of MAO (A in periphery, B in CNS)
selectively inhibits MAO-B!!!
selegiline may decrease severity of "off-on" syndrome...used in latter stages of disease
some belief that it can slow progression of parkinsons, though it ha not been confirmed
side effects...similar to other parkinsons drugs, but includes "cheese toxicity" |
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Term
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Definition
newer drug, inhibits metabolism of dopamine and l-DOPA by COMT
used in conjunction with l-DOPA
adverse affects due to increase in dopamine
hepatotoxicity is a big risk when using tolcapone
*Stalevo is a new combo drug with l-DOPA, carbidopa, and entacapone |
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Term
| Anticholinergics for treatment of Parkinsons |
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Definition
Benztropine, and trihexyphenidryl....
treatment of mild parkinsons
drugs of choice for iatrogenic parkinsonism from DA antagonists
side effects:dry mouth, dry hot skin, hyperthermia, constipation, urine retention, loss of visual acommodation, tachycardia, sedation, confusion
drug interaction with CNS depressants(alcohol, sedatives, opiods, muscle relaxants)
besides blocking muscarinic receptors, may also inhibit synaptic reuptake of dopamine |
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Term
| antihistamines for parkinsons |
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Definition
| anticholinergic activity of diphenhydramine(benedryl) |
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Term
| Other movement disorders and treament agents |
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Definition
essential tremor- propanolol, primidone, clonidine, gabapentin
Ballismus-Dopamine antagonists
Dystonia - anticholinergics, benzodiazepines, botulinium toxin
chorea - athetosis - dopamine antagonists, benzodiazepines, cholinesterase inhibitors
Tic disorders - dopamine antagonists |
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