Pharmacology Flashcards
what do competitive inhibitors change
potency of a drug. they increase Km
what do non competitive inhibitors change
they change the efficacy of a drug. they decrease Vmax
pharmacokinetics
what the body does to the drug
pharmacodynamics
what the drug does to the body
half life equation
.7 x Vd / CL
loading dose calculation
CP Vd/ F where F is bioavailability and Cp is the target plasma concentration you want
Maintenance dose calculation
Cp CL x t / F where t is the dosage interval (time between doses)
3 drugs that are zero order
PEA- this is round like a O
phenytoin, ethanol, aspirin (at very high concentrations)
drugs that are weak acids
phenobarbital, methotrexate, aspirin- give basic things like bicarbonate to trap it for an overdose.
drugs that are weak bases
amphetamines- give NH4Cl (ammonium chloride) to trap it
Therapeutic Index (TI)
TD50/ED50
sympathetic G protein classes
qiss
parasympathetic (M) G protein class
qiq
dopamine G protein class
si
histamine G protein class
qs
Vasopressin G protein class
qs
which ones use Gq
HAVe 1 M&M
which ones use Gi
M2a2D2- 2 MAD
bethanechol
direct M agonist
used for post operative ileus, and urinary retention. resistant to ache
carbachol
direct M agonist
used for glaucoma, pupillary constriction and relief of intra ocular pressure
pilocarpine
direct M agonist. potent stimulator of sweat, tears and saliva. can be used in both open and closed angle glaucoma.
methacholine
direct M agonist. this is used as a diagnostic test for asthma.
neostigmine
anticholinesterase. used for an ileus, urinary retention, MG, and reversal of NM blokade. no CNS penetration
pyridistigmine
anti cholinesterase. longer acting for MG. does not penetrate the CNS.
Physostigmine
anti cholinesterase. crosses BBB. used to reverse atropine overdose.
donepezil
anticholinesterase for Alzheimers
Rivastigmine
anticholinesterase for Alzheimers
galantamine
anticholinesterase for Alzheimers
edrophonium
this is an anti-cholinesterase. it was traditionaly used to diagnose MG. very quick acting.
organophosphates
cholinesterase inhibitor poisoning. seen in FARMERS. causes irreversible destruction of AChe. diarrhea, urination, bronchospasm, bradycardia, excitation of skeletal muscle and CNS, lacrimation, sweating, and salivation
antidote to organophosphate poisoning
need to block the ach. use atropine! you can also use pralidoxime to regenerate the Ache if given early
pralidoxime
this is a substance to regenerate the Ach e and can be used to treat organophosphoate poisoning if used early enough. complement of atropine
atropine, homatropine, and torpicamide
muscarinic antagonists.
used for the eye- produce mydriasis and cycloplegia
benztropine
muscarinic antagonists.
this is used in parkinsons disease. Park my benz
scoplamine
muscarinic antagonists.
used to treat motion sickness
Ipratropium and tiotropium
muscarinic antagonists.
used to treat COPD. should decrease airway secretions and reduce bronchoconstriction.
oxybutynin, daridenacin, and solifenacin
muscarinic antagonists.
GU. used to reduce urgency in mild cysitis and reduce bladder symptoms.
Glycopyrrolate
muscarinic antagonists.
used to reduce airway secretion and stop both drooling and gastric acid secretion.
atropine overdose
red as a beet, blind as a bat, dry as a bone, hot as a hare and mad as a hatter
Jimson weed (datura)
causes gardener’s pupil- causes mydriasis from its atropine like side effects.
epinephrine
B>A
norepi
really only used for hypotension. remember though it decreases renal perfusion a1>a2 >b1
isoproterenol
B1= B2
dobutamine
B1>B2
phenylephrine
a1>a2. this is an sympathetic agonist.
albuterol, salmeterol, terbutaline
B2>B1. these are used for COPD and asthma. terbutaline is used for premature uterine contractions.
amphetamines
indirect sympathetic agonist. also a re-uptake inhibitor and releases stored catecholamines
ephedrine
indirect sympathetic agonist. releases stored catecholamines. will increase blood pressure, decrease urinary incontinence and nasal congestion
cocaine
indirect general agonist, reuptake inhibitor.
causes vasoconstriction and local anesthesia- never give this with a beta blocker- can lead to unopposed alpha 1 activation and extreme hypertension
clonidine
alpha 2 agonist. used for hypertensive urgency. does not decrease renal blood flow. causes a decrease in sympathetic tone. can also be used for ADHD
alpha methyl dopa
this is an alpha 2 agonist. used for hypertension in pregnancy.
complication of alpha methyl dopa
coombs positive hemolytic anemia and SLE like syndrome
phenoxybenzamine
non selective alpha blocker.
used in pheochromocytoma surgery to prevent hypertensive crisis. causes orthostatic hypotension and can cause reflex tachycardia
phentolamine
non selective alpha blocker. reversible. give to patients on MAO inhibitors who eat tyramine containing foods.
beta blocker ending..
“olol” for pure beta blockers
what are beta blockers used for
angina, MI, supraventricular tachycardia (metoprolol, esmolol), hypertension (decrease CO and decrease renin secretion B1), CHF and glaucoma (decrease aqueous humor production- B2 function)
adverse outcome with metoprolol
dysplipidemia
other adverse effects of beta blockers
impotence, cardiovascular issues like bradycardia, AV block, CHF, CNS issues like seizures, sedation and sleep alterations.
which group should you NEVER give a beta blocker to
those on cociane bc will get lots and lots of lapha stimulation and ahypertensive crisis.
can you give beta blockers to diabetics
yes. some thought no because you would hide teh hypoglycemic state but beneits outweight the risk and we say go for it!
which are the beta 1 selective antagnoists
A to M- first 1/2 of the alphabet
which are the non slective beta antagonists
N to Z- second half of teh alphabet
carvedilol and labetalol
these are altered endings- means they are non selective alpha and beta blockers.
Nebivolol
B1 block (cardiac selective) with B3 stimulation which activates NO synthase in the vasculature
acetaminophen antidote
N aceylstine
this replenishes glutathione
organophosphate antidote
atropine and pralidoxine (regenerates the ache)
amphetamine antidote
NH4Cl to make the urine more acidic