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Pharmacology 1 Fall 2012
Parasympathomimetics, Beta/Alpha Blockers, Parkinson's, Sympathomimetics
83
Pharmacology
Professional
10/07/2012

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Cards

Term
Acetylcholine
Definition
Direct-Acting Muscarinic Agonist
Term
Carbachol
Definition
Direct-Acting Muscarinic Agonist

-Glaucoma
Term
Methacholine
Definition
Direct- Acting Muscarinic Agonist

-pulmonary function testing for asthma
Term
Bethanechol
Definition
Direct-Acting Muscarinic Agonist

-GI motility, Urinary Retention
Term
Pilocarpine
Definition
Direct-Acting Muscarinic Agonist

-glaucoma, xerostomia
Term
Cevimeline
Definition
Direct-Acting Muscarinic Agonist

-salivary gland dysfunction
Term
Edrophonium
Definition
-Cholinesterase Inhibitor

-Tensilon Test, diagnose myasthenia gravis

-short acting
Term
Physostigmine
Definition
Cholinesterase Inhibitor

-treat atropine or anti-muscarinic poisoning
Term
Neostigmine + Pyridostigmine
Definition
Cholinesterase Inhibitor

-myasthenia gravis, anti-nerve gas
Term
Rivastigmine
Definition
Cholinesterase Inhibitor

-Alzheimer's
Term
Echothiophate
Definition
Cholinesterase Inhibitor

-glaucoma
Term
Donepezil
Definition
Cholinesterase Inhibitor

-Alzheimer's
Term
Carbamate insecticides
Definition
Cholinesterase Inhibitor

-Irreversible, Treat only with Atropine
Term
DFP "phates"
Definition
Cholinesterase Inhibitors

-Irreversible, use atropine/pralidoxime
Term
Organophosphate (Parathion, Malathion)
Definition
Cholinesterase Inhibitors

-irreversible,use atropine/pralidoxime
Term
Sarin
Definition
Cholinesterase Inhibitor

-irreversible nerve gas
Term
Pralidoxime
Definition
Cholinesterase Reactivator

-only for organophosphates
Term
Sildenafil, Vardenafil, Tadalafil
Definition
Cyclic GMP 5 Inhibitors

-ADR: hypotension, increased heart rate
Term
Botulinium Toxin
Definition
prevents release of Acetylcholine
Term
Anticholinergic/Anti-muscarinic Drugs
Definition
competitive antagonist at muscarinic receptors

-poisoning treat with physostigmine
Term
Atropine
Definition
Antimuscarinic -prototype -CNS: low dose sedative, high dose stimulate
Term
Scopolamine
Definition
Anti-muscarinic

-CNS depressant, treats vertigo/motion sickness
Term
Dicyclomine
Definition
Anti-msucarinic

-intestinal anti-spasmodic
Term
Propantheline
Definition
Anti-muscarinic

-intestinal anti-spamodic
Term
Glycopyrrolate
Definition
Anti-muscarinic

-no CNS effect, dry respiratory secretions

-inhibit vagal reflexes
Term
Ipratropium and Tiatropium
Definition
Anti-muscarinics

-asthma and COPD
Term
Benztropine and Trihexyphenidyl
Definition
Anti-muscarinic

-Parkinson's
Term
Tolterodine, Oxybutynin, and Solifenacin
Definition
Anti-muscarinic

-Urinary incontinence
Term
Tropicamide
Definition
Anti-muscarinic

-dilates pupils
Term
Neuromuscular Blockers
Definition
work on junction to cause relaxation of paralysis of skeletal muscle
Term
Pancuromium
Definition
Neuromuscular Blocker

-non-depolarizing blocker
Term
Succinylcholine
Definition
Neuromuscular Blocker

-depolarizing, cannot be overcome by cholinesterase inhibitors
Term
Peripherally-Acting Adrenergic Neuronal Inhibitors
Definition
decrease availability of NE to receptors
Term
Reserpine
Definition
Peripherally-acting Adreneric Neuronal Inhibitor

-decreases uptake of DA and NE

-treat hypertension

-irreversible, long-acting
Term
Centrally-Acting Adrenergic Neuronal Inhibitors
Definition
Stimulate A2 sites in the brain and reduce sympathetic traffic
Term
Methyldopa
Definition
Centrally-Acting Adrenergic Neuronal Inhibitor

-prodrug

-treat hypertension in pregnancy
Term
Clonidine
Definition
Centrally-Acting Adrenergic Neuronal Inhibitor

-small, absorbed thru skin

-must be tapered or rebound hypertension

-migraine, ADHD, PTSD, drug withdrawal
Term
Guanfacine
Definition
Centrally-Acting Adrenergic Neuronal Inhibitor

-lowers cholesterol, less sedation

-treats ADHD
Term
Ganglionic Stimulants and Blockers
Definition
Act on neuronal NICOTINIC receptors

Low dose stimulant, high dose depressant
Term
Nicotine
Definition
Ganglionic Nicotinic Stimulant/Blocker

-low dose stimulant, high dose depressant

-adrenergic agonists can help treat high dose blockade
Term
Direct Acting Sypathomimetics (Adrenergic Receptor Agonists)
Definition
Alphas Constrict, Betas Dilate

-tolerance, rebound common
Term
Epinephrine
Definition
Non-selective Adrenergic Agonist

-stimulates A and B receptors
Term
Norepinephrine
Definition
Non-selective Adrenergic Agonist

-stimulates A and B1, not B2

-reflex bradycardia

-Neurogenic shock: stimulates both heart and blood vessels

-Sepsis: early "warm" phase can reverse vasodilation
Term
Isoproterenol
Definition
Non-selective Adrenergic Agonist

-stimulates betas, not used in asthma anymore

-diagnoses unexplained syncopes
Term
Dopamine
Definition
Non-selective Adrenergic Agonist

-low dose (dopamine receptors), medium dose (beta1), high (Alpha1)

-Neurogenic shock (stimulates both heart and blood vessels)

-Sepsis: "warm"=vasoconstrictor (A1), "cold"=reverse low CO (B1 stimulated)
Term
Dobutamine
Definition
Selective B1 Agonist

-increases cardiac contractility, stimulates heart during surgery

Cardiac Shock: stimulates Beta1

Sepsis: "cold"=reverse low CO
Term
Albuterol
Definition
Selective B2 agonist

-Treat bronchoconstriction in asthma and COPD, exercise induced bronchospasms
Term
Metaproterenol
Definition
Selective B2 agonist

-Treat bronchoconstriction in asthma and COPD, exercise induced bronchospasms
Term
Pirbuterol
Definition
Selective B2 agonist

-Treat bronchoconstriction in asthma and COPD, exercise induced bronchospasms
Term
Salmeterol
Definition
Selective B2 agonist

-Treat bronchoconstriction in asthma and COPD, exercise induced bronchospasms

-longest acting
Term
Terbutaline
Definition
Selective B2 agonist

-prevent premature labor by causing uterine relaxation
Term
Phenylephrine
Definition
Selective A1 agonist

-more reflex bradycardia, increased BP

-maintains diastolic and mean BP in neurogenic shock (blood vessels only)

-nasal decongestant, mydriatic agent, hemorrhoids
Term
Midodrine
Definition
Selective A1 agonist

-orthostatic hypotension
Term
Cocaine
Definition
Indirect Acting Sympathomimetic

-inhibits reuptake of NE (constricts BV at local site)

-not effective orally
Term
Pseudoephedrine
Definition
Indirect-Acting Sympathomimetic

-stimulates release of NE independent of action potentials

-treats nasal congestion and promotes sinus drainage
Term
Beta blockers
Definition
cleared by liver

-may aggravate Raynaud's or cause exercise intolerance

-may have severe hypoglycemic reaction to insulin

-sudden withdrawal causes rebound hypertension and angina
Term
Selective B1 Blockers
Definition
decrease HR and contractility, treat hypertension

-decrease conduction velocity of AV node

-prevent "thyroid storm" in hyperthyroidism
Term
Acebutolol
Definition
Selective B1 Blocker
Term
Atenolol
Definition
Selective B1 Blocker
Term
Esmolol
Definition
Selective B1 Blocker

-metabolized by ESTERASES

-short duration
Term
Metoprolol
Definition
Selective B1 Blocker
Term
Nadolol
Definition
Non-selective B1 and B2 blocker

-long acting
Term
Pindolol
Definition
Non-Selective B1 and B2 Blocker

-partial agonist
Term
Propranolol
Definition
Non-selective B1 and B2 Blocker
Term
Timolol
Definition
Non-selective B1 and B2 Blocker
Term
Labetalol
Definition
Non-selective B and Selective A1 Blocker

-treats SEVERE hypertension
Term
Alpha Blockers
Definition
Inhibitions of peripheral A-receptors

-ADR: too much loss of A-receptors (congestion, reflex tachycardia, fluid retention, hypotension)
Term
Phenoxybenzamine
Definition
Non-selective A-Blocker

-noncompetitive, irreversible (long-acting)

-prevent hypertension in pheochromocytoma PRIOR to surgery

-toxic, bad ADRs
Term
Phentolamine
Definition
Non-selective Alpha Blocker

-diagnose pheochromocytoma, short acting, given DURING surgery

-treat vasoconstriction, prevent dermal tissue necrosis

-reverse oral soft tissue anesthesia
Term
Prazosin
Definition
Selective A1 Blocker

-mild to moderate hypertension with diuretic

-treat BPH, Raynaud's, nightmares with PTSD

-ADR: first dose phenomenon of hypotension
Term
Doxazosin and Terazosin
Definition
Selective A1 Blocker

-long half-life, not for PTSD
Term
Tamsulosin and Silodosin
Definition
Selective A1 Blocker

-subgroup A1A found on bladder, less systenic ADRs

-treat BPH
Term
Alfuzosin
Definition
Selective A1 Blocker

-treat BPH, not sub-type selective

-"uroselectivity" accumulates in prostatic tissue
Term
Parkinson's and Other movement disorders
Definition
-blocking dopamine in the striatum of the brain by anti-psychotics can cause Parkinson's (reserpine and metoclopramide)

-Clozapine: treatment of psychotic effects of Dopa Drugs
Term
L DOPA
Definition
Dopaminergic Agent

-dopamine precursor, not given alone

-does not halt progression,

-"end of dose phenomenon"

-ADR:nausea, hypotension, tachycardia
Term
L DOPA/ Carbidopa (Sinemet)
Definition
Dopaminergic Agent

-inhibits DOPA decarboxylase in periphery
Term
L DOPA/Carbidopa/Entacapone
Definition
Dopaminergic Agent

-inhibits metabolism of dopamine by COMT
Term
Bromocriptine
Definition
Dopaminergic Agent -not as effective as DOPA -not approved to inhibit prolactin secretion anymore -used with L DOPA but with additive side-effects
Term
Pramipexole and Ropinirole
Definition
Dopaminergic Agent

-D2 and D3 receptors

-may have antioxidant and neuroprotective effects which may slow progression
Term
Amantadine
Definition
Dopaminergic Agent

-stimulate release of dopamine
Term
Selegiline/Deprenyl
Definition
MAO-B Inhibitor

-inhibit metabolism of dopamine by MAO-B in CNS

-studies do not confirm that it slows progression

-ADR: "cheese toxicity"
Term
Benztropine and Trihexyphenidyl
Definition
COMT inhibitor

-more effective against tremors

-treatment of iatrogenic Parkinson's due from DA antagonists
Term
Diphenhydramine
Definition
Antihistamine

-due to anti-cholinergic effect
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