Term
Neuromuscular blocking agents MOA |
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Definition
Block acetylcholine from activating nicotinicM receptors on skeletal muscles Cause muscle relaxation |
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Term
Neuromuscular blocking agents Uses |
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Definition
Surgery for muscle relaxation Endotracheal intubation Mechanical ventilation Other diagnostic procedures |
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Term
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Definition
Nondepolarizing Neuromuscular Blockers II
Intermediate-acting agents – duration 20-40 min. |
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Term
Succinylcholine (Anectine) |
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Definition
Mechanism of action –Binds to Nicotinic – M receptors on the motor end plate of muscle.
Pharmacologic effects Muscle relaxation – flaccid paralysis Central nervous system- no effect Pharmacokinetics – peak 1min, duration 4-10 min. Ultra short acting drug. Therapeutic uses- EET
Adverse effects Prolonged apnea in patients with low pseudocholinesterase activity Malignant hyperthermia Postoperative muscle pain – neck & shoulders Hyperkalemia
Drug interactions Cholinesterase inhibitors – potentiate effects Antibiotics- intensify effects Toxicology Preparations, dosage, and administration – 25-75mg IV |
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Term
Therapeutic Uses of Neuromuscular Blockers |
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Definition
Muscle relaxation during surgery Facilitation of mechanical ventilation Adjunct to electroconvulsive therapy Endotracheal intubation Diagnosis of myasthenia gravis |
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Term
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Definition
Nondepolarizing Neuromuscular Blockers II Intermediate-acting agents – duration 20-40 min. |
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Term
Therapeutic Applications of Alpha1 Activation |
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Definition
Hemostasis (vasoconstriction) Nasal decongestion Adjunct to local anesthesia – delays anesthesia absorption Elevation of blood pressure (vasoconstriction) Mydriasis (dilatation of pupil) |
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Term
Adverse Effects of Alpha1 Activation |
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Definition
Hypertension Necrosis Bradycardia |
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Term
Therapeutic Application of Beta1 Activation |
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Definition
Cardiac arrest Heart failure Shock AV heart block |
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Term
Adverse Effects of Beta1 Activation |
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Definition
Altered heart rate or rhythm Angina pectoris |
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Term
Therapeutic applications of beta2 activation |
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Definition
Asthma – terbutaline inhalation Delay of preterm labor |
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Term
Adverse Effects of Beta2 Activation |
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Definition
Hyperglycemia – only in DM Tremor – most common due to skeletal muscle contractions |
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Term
Clinical Consequences of Dopamine Receptor Activation |
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Definition
Activation of peripheral dopamine receptors causes dilation of the vasculature of the kidneys. Dopamine is only drug to activate dopamine receptors |
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Term
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Definition
Receptor specificity - alpha1, alpha2, beta1, beta2. Therapeutic uses- pg. 157 Adverse effects Hypertensive crisis – alpha 1 Dysrhythmias – beta 1 Angina pectoris – beta 1 Necrosis following extravasation Hyperglycemia – beta 2 in DM
Drug interactions MAO inhibitors Tricyclic antidepressants General anesthetics Alpha-adrenergic blocking agents Beta-adrenergic blocking agents Preparations, dosage, and administration – any route |
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Term
Norepinephrine (Levophed) |
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Definition
Receptor specificity Alpha1,Alpha2, Beta1 Chemical classification Catecholamine Adverse effects Hypertensive crisis – alpha 1 Dysrhythmias – beta 1 Angina pectoris – beta 1 Necrosis following extravasation **Clinical applications = hypotensive states & cardiac arrest. IV ONLY |
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Term
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Definition
Receptor specificity: beta1 and beta2 Chemical classification: catecholamine Therapeutic uses Cardiovascular – AV block, Inc. cardiac output, shock. Asthma – bronchodilation although has been abandoned due to cardiac effects. Bronchospasm Adverse effects – tachydysrhythmias, angina pectoris, hyperglycemia. Drug interactions- MAO Inhibitors Preparations and administration – 0.2-0.02 mg/ml |
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Term
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Definition
Receptor specificity: dopamine, beta1, (high doses) alpha1 Therapeutic uses Shock Heart failure Acute renal failure ??? Adverse effects – tachycardia, dysrhythmias, & anginal pain Drug interactions - MAO Inhibitors Preparations, dosage, and administration Preparations: is dispensed in aqueous solutions Dosage: must be diluted Administration: administered by IV, 2-5 mcg/kg/min |
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Term
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Definition
Receptor specificity: beta1 Chemical classification: catecholamine Actions and uses – heart failure Adverse effects – Tachycardia, monitor BP and ECG. Drug interactions - MAO Inhibitors Preparations, dosage, and administration Preparations: is dispensed in aqueous solutions Dosage: must be diluted Administration: administered by IV, 2.5 - 10 mcg/kg/min |
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Term
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Definition
Receptor specificity: beta2 Chemical classification: noncatecholamine Therapeutic uses Asthma Delay of preterm labor Adverse effects Tremor & Tachycardia Minimal at therapeutic doses |
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Term
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Definition
Direct blockade of adrenergic receptors |
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Term
Alpha-adrenergic blocking agent Uses |
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Definition
Therapeutic Essential hypertension Benign prostatic hyperplasia hyperplasia (BPH) (decrease contraction of smooth muscle in bladder) Raynaud’s disease – peripheral vascular disorder with vasospasms in the toes and fingers. Overdose of alpha1 agonist |
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Term
Alpha-adrenergic blocking agent |
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Definition
Nonselective Produces alpha1 and alpha2 blockade
Selective Produces alpha1 blockade |
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Term
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Definition
Alpha-Adrenergic Blocking Agents
Selective Produces alpha1 blockade
Actions and uses – dilation of arterioles & veins, relaxation of smooth muscles & prostatic capsule. Pharmacokinetics – peak 1-3 hours, duration 10 hours. Adverse effects – Orthostatic hypotension, reflex tachycardia. Preparations, dosage, and administration – (1,2, & 5 mg tabs) Adult dose 1mg bid. |
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Term
Alpha-1 Blockade Adverse Effects |
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Definition
Orthostatic hypotension Reflex tachycardia Nasal congestion Inhibition of ejaculation – sexual dysfunction (nonadherence) Sodium retention and increased blood volume – may see lasix in conjunction with this type of med. |
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Term
Orthostatic hypotension Reflex tachycardia Nasal congestion Inhibition of ejaculation – sexual dysfunction (nonadherence) Sodium retention and increased blood volume – may see lasix in conjunction with this type of med. |
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Definition
The most significant adverse effect associated with alpha2 blockade is potentiation of the reflex tachycardia. |
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Term
Beta-Adrenergic Blocking Agents |
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Definition
Nonselective Blocks beta1 and beta2 receptors
Cardioselective Blocks beta1 receptors |
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Term
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Definition
Cardioselective blocks beta 1 Pharmacologic effects - dec. HR& dec. CO. but does not block bronchial beta 2 receptors. Pharmacokinetics – lipid soluble Therapeutic uses - HTN Adverse effects – Bradycardia, AV heart block, Heart failure, Rebound cardiac excitation Precautions, warnings, and contraindications – Sinus brady, heart failure. Safer with asthma & DM Preparations, dosage, and administration – 50-100mg QD. |
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Term
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Definition
Nonselective beta 1 & beta 2 Pharmacologic effects – dec. HR& dec. CO Pharmacokinetics – highly lipid soluble Therapeutic uses – HTN, angina, MI Adverse effects Bradycardia AV heart block Heart failure Rebound cardiac excitation
Bronchoconstriction Inhibition of glycogenolysis CNS effects – derpession, insomnia, nightmares, & hallucinations Precautions, warnings, and contraindications Severe allergy – avoid Diabetes – masks hypoglycemia and Tachycardia (defense mechanism) Cardiac, respiratory, and psychiatric disorders
Drug interactions Calcium channel blockers – same effects Insulin Preparations, dosage, and administration General dosing considerations Preparations – (10-90 mg) Dosage – (40 mg BID) |
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Term
Beta-Adrenergic Antagonists I: Therapeutic Responses to Beta Blockade |
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Definition
(reduced heart rate, reduced force of contraction, & reduced velocity of impulse)
Therapeutic applications of beta blockade: Angina pectoris – decrease cardiac work. Hypertension & Cardiac dysrhythmias – reduce PVR. Myocardial infarction – reduces pain and infarct size Heart failure Hyperthyroidism Migraine Stage fright Pheochromocytoma – large amt. of catecholamines Glaucoma |
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Term
Beta-Adrenergic Antagonists I: Adverse Responses to Beta Blockade |
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Definition
Adverse effects of beta blockade involve both beta1 and beta2 blockade. Adverse effects of beta1 blockade: most common Bradycardia Reduced cardiac output –use with caution in heart failure Precipitation of heart failure AV heart block Rebound cardiac excitation – do not stop abruptly! Adverse effects of beta2 blockade: Bronchoconstriction – contraindicated with Asthma. Inhibition of glycogenolysis – may cause hypoglycemia |
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Term
Parasympathetic Nervous System (PSNS)
The regulatory functions of PNS affect these sites |
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Definition
Heart rate- slows down Gastric secretions - Increased Bladder and bowel - Empties Vision – focuses the eyes for near vision (constricts pupil) Bronchial smooth muscle - contracted |
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Term
Parasympathetic Nervous System (PSNS) |
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Definition
Conserves Energy (by releasing the cholinergic neurohormone acetylcholine) |
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Term
Sympathetic Nervous System |
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Definition
Controls energy expenditure in stressful situations by releasing the adrenergic catecholamine norepinephrine |
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Term
Main functions of the Sympathetic Nervous System |
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Definition
Regulation of cardiovascular system Regulation of body temperature Implementation of “fight or flight” reaction |
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Term
Neurotransmitters of the Peripheral Nervous System (PNS) |
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Definition
Acetylcholine Norepinephrine Epinephrine Dopamine |
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Term
Cholinergic receptor mediated by ? |
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Definition
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Term
Adrenergic receptors mediated by? |
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Definition
norepinephrine and epinephrine |
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Term
Dopamine Receptor mediated by? |
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Definition
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Term
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Definition
A molecular structure within a cell or on the surface characterized by: Selective binding of a specific substance Specific physiologic effect that accompanies the binding (like neurotransmitters) |
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Term
Adrenergic Receptor (Alpha and Beta) |
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Definition
Sites on effector organs innervated by postganglionic adrenergic fibers of the SNS, classified as Alpha and Beta adrenergic receptors according to their reaction to norepinephrine and epinephrine, respectively, and to certain blocking and stimulating agents |
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Term
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Definition
Adrenergic receptors that respond particularly to epinephrine and to such blocking agents as propanolol. Subdivided into Beta 1 and Beta 2, and Beta 3 (atypical) |
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Term
Cholinergic Receptor (Muscarinic and Nicotinic) |
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Definition
Cell-surface receptors that bind the neurotransmitter acetylcholine and mediate its action on postjunctional cells, including parasympathetic autonomic effector cells, sympathetic and parasympathetic autonomic ganglion cells, striated muscle, and certain central neurons |
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Term
Subtypes of Cholinergic receptors |
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Definition
Nicotinic n Nicotinic m Muscarinic |
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Term
Subtypes of adrenergic receptors |
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Definition
Alpha1 and alpha2 Beta1 and beta2 Dopamine |
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Term
Nicotinic n (neuronal)receptor function |
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Definition
Promotes ganglia transmission Promotes release of epinephrine |
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Term
Nicotinic m (muscle) receptor function |
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Definition
Contraction of skeletal muscle |
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Term
Muscarinic receptor function |
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Definition
Activates parasympathetic nervous system |
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Term
Alpha1 receptor function (adrenergic) |
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Definition
Vasoconstriction Ejaculation Contraction of bladder neck and prostate |
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Term
Alpha2 receptor function (adrenergic) |
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Definition
Located in presynaptic junction Minimal clinical significance Mediator of Negative Feedback preventing further release of Nor-epi |
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Term
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Definition
Bronchial dilation Relaxation of uterine muscle Vasodilation Glycogenolysis (Inc. Blood sugar in DM) |
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Term
Dopamine receptor function |
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Definition
Dilates renal blood vessels |
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Term
Epinephrine receptor specificity |
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Definition
can activate all alpha and beta receptors, but not dopamine receptors |
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Term
Norepinephrine specificity |
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Definition
can activate alpha1, apha2, and beta1, receptors, but not beta2 or dopamine receptors. |
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Term
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Definition
can activate alpha1, beta1, and dopamine receptors.
Dopamine is the only neurotransmitter capable of activating dopamine receptors. |
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Term
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Definition
A drug that has an affinity for and stimulates physiologic activity at cell receptors normally stimulated by naturally occurring substances |
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Term
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Definition
A substance that tends to nullify the action of another, as a drug that binds to a cell receptor without eliciting a biological response, blocking binding of substances that could elicit such responses |
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Term
Muscarinic Antagonist (Anticholinergic/parasympatholytic) |
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Definition
Drug that blocks the action of acetylcholine at muscarinic receptors
e.g. atropine |
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Term
Muscarinic Antagonist (Atropine) Characteristics |
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Definition
Actions Increases heart rate Decreases secretions Relaxes bronchi Decreases bladder tone Decreases GI tone and motility Dilates the pupil CNS excitation
Uses – Preanesthestic Disorders of the eye Bradycardia Intestinal hypertoxicity and hypermotility Muscarinic agonist poisoning Asthma – Biliary colic Peptic ulcer disease
Adverse effects Dry mouth (xerostomia) Blurred vision Photophobia Increased intraocular pressure Urinary retention Constipation Tachycardia – Anhydrosis – Asthma
Drug interactions Avoid combining atropine with other drugs capable of causing muscarinic blockade. (antihistamines, antipsychotics, & tricyclic antidepressants) Preparations, dosage, and administration 0.4 mg tab or 0.05-1mg/ml. Average adult dose = 0.5mg |
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Term
Muscarinic Agonists (Parasympathomimetic) |
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Definition
Uses Urinary retention GERD Ileus Postoperative abdominal distention Glaucoma
Adverse effects Exacerbation of asthma |
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