Pharmacology Flashcards
Efficacy
Maximal effect a drug can produce.
Potency
Amount of drug needed for a given effect
Bethanechol
cholinomimetic agent (acts like ACh) , direct agonist
Activates bladder smooth muscle
urinary retention
Carbachol
cholinomimetic agent (acts like ACh), direct agonist constricts pupil and relieves intraocular pressure in open-angle glaucoma
Methacholine
cholinomimetic agent (acts like ACh), direct agonist
Stimulated muscarinic receptors in airway when inhaled
challenge test for diagnosis of asthma
Pilocarpine
cholinomimetic agent (acts like ACh), direct agonist potent stimulator of sweat, tears and saliva
Donepezil
cholinomimetic agent, indirect agonist
1st line for Alzheimer disease
penetrate the CNS
Rivastigmine
cholinomimetic agent, indirect agonist
1st line for Alzheimer disease
penetrate the CNS
Galantamine
cholinomimetic agent, indirect agonist
1st line for Alzheimer disease
penetrate the CNS
Edrophonium
cholinomimetic agent, indirect agonist
Historically used to diagnose myasthenia gravis; replaced by anti-AChR Ab (anti-acetylcholine receptor antibody) test
quaternary amine
diagnostic tool (tensilon test)
Neostigmine
cholinomimetic agent, indirect agonist
Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative)
antibody) test
quaternary amine
Physostigmine
cholinomimetic agent, indirect agonist
antidote for anticholinergic toxicity
DUMBBELS : diarrhea, urination, miosis, bronchospasm, bradycardia, lacrimation, salivation
Pyridostigmine
cholinomimetic agent, indirect agonist
myasthenia gravis (long acting); does not penetrate CNS (antibody) test
quaternary amine)
Atropine
Muscarinic antagonists treats peripheral and central toxicity Jimson Weed & Belladonna flower Mydriasis, cycloplegia Tachycardia Suppressed sweating = hyperthermia Dry mouth and eyes Blurred vision BE CAREFUL WITH ELDERLY - ALICE TEA PARTY
Homatropine
Muscarinic antagonists
Tropicamide
Muscarinic antagonists
Benztropine
Muscarinic antagonists
M1 ( think Parkinson’s = deficient dopamine & excess ACh ) CNS reduce tremors and rigidity
Trihexyphenidyl
Muscarinic antagonists
M1 ( think Parkinson’s = deficient dopamine & excess ACh) CNS reduce tremors and rigidity
Glycopyrrolate
Muscarinic antagonists
Hyoscyamine
Muscarinic antagonists
Dicyclomine
Muscarinic antagonists
Ipratroprium
Muscarinic antagonists
M3 - bronchodilator
Tiotropium
Muscarinic antagonists
M3 - bronchodilator
Oxybutynin
Muscarinic antagonists
M3 - hold your pee
Solifenacin
Muscarinic antagonists
Tolterodine
Muscarinic antagonists
M3 - hold your pee
Scopolamine
Muscarinic antagonists (inhibits M1 CNS) Used to treat sea sickness (patch)
Albuterol
Direct Sympathomimetic
BETA 2 AGONIST
Acute asthma
Salmeterol
Direct Sympathomimetic
BETA 2 AGONIST
Terbutaline
Direct Sympathomimetic
BETA 2 AGONIST
dilate smooth muscle - relaxes the uterus
Dobutamine
Direct Sympathomimetic
BETA 1 AGONIST, little beta 2
Heart ramp up
increase pulse pressure = increase systolic, decrease diastolic
Dopamine
Direct Sympathomimetic
D1 Gs increased cAMP beta1 then alpha1
D2 Gi CNS
Epinephrine
Direct Sympathomimetic
Blood to target tissues - acts as hormone
BETA more then alpha
low dose BETA effects
Fenoldopam
Direct Sympathomimetic
Isoproterenol
Direct Sympathomimetic
BETA 1 & 2 AGONIST
diastolic drop beta 2
Midodrine
Direct Sympathomimetic
Mirabegron
Direct Sympathomimetic
Norepinephrine
Direct Sympathomimetic
activate Adrenergic receptors on post synaptic cells - acts as neurotransmitter
alpha 1 & 2 AGONIST (some beta) increase PP
treat septic shock
Phenylephrine
Direct Sympathomimetic ALPHA 1 AGONIST used as a nasal decongestant maintain CO, increase MAP reflex bradycardia treat septic shock
Amphetamine
Indirect Sympathomimetic
Displace catecholamines into synapse
Cocaine
Indirect Sympathomimetic
Inhibits NET and DAT. Build up of catecholamines in synapse. vasoconstrictor
never give beta blocker
Ephedrine
Indirect Sympathomimetic
Adrenergic
Epinephrine/Norepinephrine is the neurotransmitter
Cholinergic
Acetylcholine is the neurotransmitter
alpha 1
adrenoreceptor (Epi/NE)
Gq = Phospholipase C, IP3/DAG, increased intracellular Ca2+
Vascular smooth muscle of the skin, skeletal muscle, and the splanchnic region, in the sphincters of the gastrointestinal tract and bladder, and in the radial muscle of the iris
VASOCONSTRICTION/VENOCONSTRICTION
alpha 2
adrenoreceptor (Epi/NE)
Gi = Adenylate cyclase inhibitor
Gastrointestinal tract, wall, decrease insulin release
VASODILATION
beta 1
HEART
adrenoreceptor (Epi/NE)
Gs = Adenylate cyclase stimulator
Heart, salivary glands, adipose tissue, kidney
INCREASED HEART RATE - cardiac myocytes including SA and AV nodes
increased renin
beta 2
adrenoreceptor (Epi/NE) Gs = Adenylate cyclase stimulator Vascular smooth muscle of skeletal muscle, walls of gastrointestinal tract and bladder, bronchioles BRONCHODILATION DROP IN DIASTOLIC PRESSURE LIPOLYSIS GLUCONEOGENESIS INCREASED INSULIN
M1
cholinergic (ACh)
nerves in the CNS
Gq = Phospholipase C, IP3, increased intracellular Ca2+
M2
cholinergic (ACh)
myocardium and smooth muscle
Gi = Adenylate cyclase inhibitor
RELAXATION
M3
cholinergic (ACh)
glands, bladder, smooth muscle of the eye
Gq = Phospholipase C, IP3, increased intracellular Ca2+
CONTRACTION
nonselective alpha 1, alpha 2
phenoxybenzamine (irreversible)
used in pheochromocytoma
Phentolamine (reversible)
used to reverse the cheese effect (block breakdown of tyramine)
Myasthenia Gravis
Autoimmune disease. Antibodies block ACh receptors. Repetitive movements decrease ACh levels, problem worsens.
Eye problems. Chewing, talking, swallowing problems.
Endrophonium/Tensilon test (drug prevents the breakdown of ACh)
Lambert-Eaton Syndrome
Paraneoplastic syndrome (small cell lung cancer) Antibodies against pre-synaptic Ca channels (prevent ACh release) Endrophonium/Tensilon test (drug prevents the breakdown of ACh): no improvement
Succinylcholine
cholinomimetic agent, indirect agonist
depolarizing neuromuscular blocking agent
Phase-1 block
Brimonidine
alpha 2 agonist
used to treat chronic open angle glaucoma (decreases aqueous humor production)
metyrosine
Indirect Sympathomimetic
Prevents conversion of tyrosine to L-DOPA
atomoxetine
Indirect Sympathomimetic
Used to treat ADHD
NET inhibitor
reserpine
Indirect Sympathomimetic
inhibits VMAT, depleting neurotransmitter stores
methylphenidate
Indirect Sympathomimetic
an amphetamine derivative (Displace catecholamines into synapse)
used to treat ADHD
modafinil
Indirect Sympathomimetic
stimulate used to treat narcolepsy
clonidine
alpha 2 agonist
CNS reduces BP
reduced sympathetic tone
used to treat ADHD, tourette’s
tizanidine
alpha 2 agonist
muscle relaxant
phentolamine
alpha 1 and alpha 2 antagonist REVERSIBLE
vasodilation
used to treat cocaine toxicity
used during surgery (short acting)
phenoxybenzamine
alpha 1 and alpha 2 antagonist IRREVERSIBLE
used days before surgery
prazosin, terazosin, doxazosin, tamsulosin
-osin
alpha 1 selective antagonists
smooth muscle relaxation
mirtazapine
alpha 2 antagonist
antidepressant
Atenolol, Betaxolol, Esmolol, Acebutolol, Metoprolol
Beta 1 selective antagonists
cardio selective
Carvedilol
non selective beta 1 antagonists
and alpha 1 blocker
labetalol
nonselective beta blocker and alpha 1 blocker
treats hypertension in pregnancy
hypertensive emergency
esmolol
beta blocker
treat hypertensive emergency