Pharmacolgy Flashcards
Briefly describe additive, synergistic and permissive effects
Additive - A w/ B = A + B. Synergistic - A w/ B > A + B. Permissive - B = 0 but A w/ B > A
Formula for volume of distribution
[Amount of drug in body] / [plasma dug concentration]
Formula for half life
(0.7 x Vd) / CL
Formula for loading dose
Cp x Vd/F. Cp is desired peak concentration, Vd is volume of distribution. F is bioavailability
Drugs that undergo zero order elimination
Phenytoin, Ethanol, Aspirin (very high dosese)
What type of compounds preferentially get metabolized by the liver?
Lipophilic compounds
On a dose response curve, which axis is potency and which is efficacy?
Potency is x axis, efficacy is y axis
What relationship do norepinephrine and phenoxybenzamine have at alpha receptors?
Noncompetitive antagonist
What type of receptors are nicotinic receptors?
Ligand-gated Na/K channels
G protein class for the sympathetic receptors
A1 - q, A2 - i, B1 - s, B2 - s
G protein class for the parasympathetic receptors
M1 - q, M2 - i, M3 - q
G protein class for dopamine, histamine, and vasopressin receptors
D1 - s, D2 - i. H1 - q, H2 - s. V1 - q, V2 - s
Gq receptors
Use phospholipase C to create PIP2 which creates DAG (PKC) and IP3 (Ca influx)
Gs receptors
Stimulate adenylyl cyclase to increase cAMP levels, which increases PKA levels, which increases Ca influx (heart) and inhibits MLCK (SM)
Gi receptors
Inhibit adenylyl cyclase levels, decreasing cAMP
Which sympathetic receptor does NE not act much on?
B2
How can you tell the difference between an alpha agonist and a muscarinic antagonist?
Alpha agonism causes mydriasis, muscarinic antagonism causes mydriasis AND FLUSHING
Direct cholinomimetic agents
Bethanechol, carbachol, pilocarpine, methacholine
Indirect cholinomimetics (AChE-Is)
Neostigmine, pyridostigmine, edrophonium, physostigmine, echothiophate, donepezil
What do organophosphates do biochemically?
Shut down AChE
Treatment for organophosphate poisoning and rationale
Atropine to help muscarinic receptors, pralidoxime to help nicotinic receptors (muscle paralysis)
Pralidoxime
Regenerates active AChE. Give with atropine in cholinesterase poisoning
Muscarinic antagonists
Eye - atropine, homatropine, tropicamide. CNS - benztropine, scopolamine. Respiratory - ipratropium. GU - oxybutynin, glycopyrrolate. GI - methscopolamine, pirenzepine, propantheline
Tiotropium
Trade name spiriva. Muscarinic antagonist used in asthma and COPD
Which sympathetic receptors does epi act at?
A1, A2, B1, B2 (all of them except D1)
Isoproterenol
B1 and B2 agonist. Used in AV block
Which sympathetic receptors does dopamine act at?
High dose - A1 and A2. Medium dose - B1 and B2. Low dose - D1. Use in shock to increase renal perfusion
Dobutamine
B1 agonist with some activity at A1, A2, and B2. Inotropic but not chronotropic
Phenylephrine
A1 and A2 agonist (more activity at A1 than A2)
Ritodrine
Selective B2 agonist. Reduces premature uterine contractions
Action of amphetamine and ephedrine
Indirect sympathetic agonists. Release stored catecholamines
Action of cocaine
Indirect general sympathetic agonist. Uptake inhibitor
Clonidine, alpha-methyldopa
Centrally acting alpha 2 agonists. Decrease adrenergic outflow. Use in HTN with renal disease
Phenoxybenzamine
Nonselective irreversible alpha blocker. Use in pheochromocytoma
Phentolamine
Reversible nonselective alpha blocker. Give to patients on MAOIs who eat tyramine-containing foods
Prazosin, terazosin, doxasin
Alpha-1 blockers. Use in HTN, BPH