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219 Cards in this Set

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Ganciclovir (DHPG dihydroxy-2-propoxymethyl guanine)
p300
Mechanism of action of Ganciclovir.
Phosphorlation by viral kinase; perferentially inhibits CMV DNA polymerase.
Clinical use of Ganciclovir.
CMV, especially in immunocompromised patients.
Symptoms of Ganciclovir toxicity.
Leukopenia, neutropenia, thrombocytopenia, renal toxicity. More toxic to host enzymes than acyclovir.
Foscarnet
p300
Mechanism of action of Foscarnet.
Viral DNA polymerase inhibitor that binds to the pyrophophate binding site of the enzyme. Does not require activation by viral kinase. "FOScarnet = pyroFOSphate analog."
Clinical use of Foscarnet.
CMV retinitis in immunocompromised patients when ganciclovir fails.
Symptoms of Foscarnet toxicity.
Nephrotoxicity.
HIV therapy
p300
Saquinavir, ritonavir, indinavir, nelfinavir, amprenavir are example of this type of anti-HIV drug.
Protease inhibitor.
Mechanism of action of protease inhibitors.
Inhibit assembly of new virus by blocking protease enzyme.
Symptoms of protease inhibitor toxicity.
GI intolerance (nausea, diarrhea), hyperglycemia, lipid abnormalities, thrombocytopenia (indinavir).
Reverse transcriptase inhibitors:

Zidovudine (AZT), didanosine (ddI), zalcitabine (ddC), stavudine (d4T), lamivudine (3TC), and abacavir are examples of --------- reverse transcriptase inhibitors.
Nucleoside.
Nevirapine, delavirdine, and efavirenz are examples of --------- reverse transcriptase inhibitors.
Non-nucleoside.
Mechanism of action of reverse transcriptase inhibitors.
Preferentially inhibit reverse transcriptase of HIV; prevent incorporation of viral genome into host DNA.
Symptoms of reverse transcriptase inhibitor toxicity.
Bone marrow supression (neutropenia, anemia), periphral neuropathy, lactic acidosis (nucleosides), rash (non-nucleosides), megaloblastic anemia (AZT).
Highly active antiretroviral therapy (HAART) generally entails combination therapy with ---------- and -----------.
Protease inhibitors, reverse transcriptase inhibitors.
When should HIV therapy be initiated?
When patients have low CD4 counts (<500 cells/mm3) or high viral load.
-------- is used during pregnancy to reduce risk of fetal transmission.
AZT.
Interferons
p300
Mechanism of action of Interferons.
Glycoproteins from human leukocytes that block various stages of viral RNA and DNA synthesis.
Clinical use of Interferons.
Chronic hepatitis B and C, Kaposi's sarcoma.
Symptoms of Interferon toxicity.
Neutropenia.
Antiparasitic drugs
p301
Clinical uses of Ivermectin.
Onchocerciasis "rIVER blindness treated with IVERmectin".
Clinical uses of Mebendazole / thiabendazole.
Nematode/roundworm (e.g., pinworm, whipworm) infections.
Clinical uses of Pyrantel pamoate.
Giant roundworm (Ascaris), hookworm (Necator/Ancylostoma), pinworm (Enterobius).
Clinical uses of Praziquantel.
Trematode/fluke (e.g., schistosomes, Paragonimus, Clonorchis) and cysticercosis.
Clinical uss of Niclosamide
Cestode/tapeworm (e.g., Diphyllobothrium latum, Taenia species) infections except cysticercosis.
Clinical uses of Pentavalent antimony.
Leishmaniasis.
Clinical uses of Chloroquine, quinine, mefloquine, atovaquone, proguanil.
Malaria.
Clinical uses of Primaquine.
Latent hypnozoite (liver) forms of malaria (Plasmodium vivax, P.ovale).
Clinical uses of Metronidazole.
Giardiasis, amebic dysentery (Entamoeba histolytica), bacterial vaginitis (Gardnerella vaginalis), Trichomonas.
Clinical uses of Pentamidine.
Pneumocystis carinii pneumonia prophylaxis.
Clinical uses of Nifurtimox.
Chagas' disease, American trypanosomiasis (Trypanosoma cruzi).
Clinical uses of Suramin.
African trypanosomiasis (sleeping sickness).
Pharmacology - CNS / Neurologic drugs
p301
Parasympathetic preganglionic neurons release the neurotransmitter -------- which act on -------- receptors.
Ach, nicotinic.
Parasympathetic postganglionic neurons release the neurotransmitter -------- which act on ------- receptors.
Ach, muscarinic.
Sympathetic preganglionic neurons to sweat glands release the neurotransmitter ------- which act on ------- receptors.
Ach, nicotinic.
Sympathetic postganglionic neurons to sweat glands release the neurotransmitter ------- which act on ------- receptors.
Ach, muscarinic.
Sympathetic preganglionic neurons to glands, cardiac and smooth muscles release the neurotransmitter ------- which act on ------- receptors.
Ach, nicotinic.
Sympathetic postganglionic neurons to glands, cardiac and smooth muscles release the neurotransmitter ------- which act on ------- receptors.
NE, alpha and beta
Sympathetic preganglionic neurons to renal vascular smooth muscle release the neurotransmitter ------- which act on ------- receptors.
Ach, nicotinic.
Sympathetic postganglionic neurons to renal vascular smooth muscle release the neurotransmitter ------- which act on ------- receptors.
Dopamine, D1
Sympathetic preganglionic neurons to the adrenal medulla release the neurotransmitter ------- which act on ------- receptors.
Ach, nicotinic.
Sympathetic preganglionic neurons to the adrenal medulla synapse directly on ------- cells of the adrenal medulla.
Chromaffin.
Somatic neurons synapse directly on -------- muscle and release the neurotransmitter ------- which act on ------- receptors.
skeletal muscle, Ach, nicotinic.
Autonomic drugs
p302
Cholinergic:

Ach is synthesized from acetyl-CoA and choline by the enzyme ---------.
Choline acetyltransferase.
The transport of choline into the nerve terminal can be inhibited by --------.
Hemicholinium.
The release of transmitter from vesicles in the nerve ending require the entry of ------ into the neuron.
Calcium.
#NAME?
Botulinum toxin.
The action of Ach in the synapse is terminated by its metabolism to acetate and choline by the enzyme ---------.
Acetylcholinesterase.
Noradrenergic:

In the noradrenergic nerve terminal, tyrosine is hydroxylated to -------, which is decarboxylated to --------, which is finally hydroxylated to NE.
DOPA, dopamine.
Dopamine is transported into vesicles for hydroxylation to NE. This transport can be blocked by the drug --------.
Reserpine.
The action of NE and DA is terminated by --------- and ----------.
Reuptake, diffusion (different than for Ach).
--------- inhibits the release of the stored NE.
Guanethidine.
The --------- drugs promote catecholamine release.
Amphetamine.
The drugs --------- and ---------- inhibit the reuptake of NE.
Cocaine, TCA.
The release of NE from a sympathetic nerve ending is modulated by ---------, --------- and ---------.
NE, Ach, angiotensin II.
NE inhibits its own release at the noradrenergic nerve terminal through --------- receptors.
Alpha 2.
Angiotensin II --------- (inhibits / stimulates) the release of NE from the noradrenergic nerve terminal.
Stimulates.
Ach inhibits the release of NE from the noradrenergic nerve terminal by binding to --------- receptors.
M1.
Cholinomimetics
p303
Direct agonists:

Clinical application and action of Bethanechol.
Postoperative and neurogenic ileus and urinary retention. / Activates bowel and bladder smooth muscle.
Clinical application and action of Carbachol and Pilocarpine.
Glaucoma. / Activates ciliary muscle of eye (open angle), pupillary sphincter (narrow angle).
Indirect agonists (anticholinesterases):

Clinical application / action of Neostigmine.
Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative). / Increase endogenous Ach.
Clinical application / action of Pyridostigmine.
Myasthenia gravis. / Increase Ach; increase strength.
Clinical application / action of Edrophonium.
Diagnosis of myasthenia gravis (extremely short acting). / Increase endogenous Ach.
Clinical application / action of Physostigmine.
Glaucoma (crosses blood-brain barrier) and atropine overdose. / Increase endogenous Ach.
Clinical application / action of Echothiophate.
Glaucoma. / Increase endogenous Ach.
Symptoms of cholinesterase inhibitor poisoning.
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation (also abdominal cramping). "DUMBBELSS".
Cholinesterase inhibitor poisoning may be caused by ---------.
Parathion and other organophosphates.
The cholinesterase regenerator ------- can be used as an antidote for cholinesterase inhibitor poisoning.
Pralidoxime.
Mechanism of action of Pralidoxime.
Regenerates active cholinesterase, chemical antagonist, used to treat organophosphate exposure.
Cholinoreceptor blockers:
p303
Clinical uses of the muscarinic antagonist Atropine.
Dilate pupils, decrease acid secretion in peptic ulcer disease, decrease urgency in mild cystitis, decrease GI motility, reduce airway secretions, and treat organophosphate poisoning. "Blocks SLUD: Salivation, Lacrimation, Urination, Defecation."
Side effects of Atropine.
Increase body temp, rapid pulse, dry mouth, dry/flushed skin, disorientation, mydriasis with cycloplegia, and constipation. "Atropine parasympathetic block side effects: Blind as bat, Red as a beet, Mad as a hatter, Hot as a hare, Dry as a bone."
Hexamethonium (ganglionic blocker) blocks -------- receptors.
Nicotinic.
AUTHOR
Tzivia Moreen
antimuscarinic drugs
p. 304
tropi are anti-muscarinic
while vacationing in the tropics you lie on a beach and your muscles waste away!
benztropine is used to treat
Parkinson's disease
scopolamine is used to treat
motion sickness
scopolamine is an antimuscarinic that does not convert to the mnemonic!

name 2 antimuscarinic drugs that act on the CNS
benztropine, scopolamine
name a muscarinic used to treat motion sickness
scopolamine
name a muscarinic used to treat Parkinson's disease
benztropine
mechanism of action of benztropine
antimuscarinic
mechanism of action of scopolamine
antimuscarinic
name three antimuscarinics that act on eye
atropine, homatropine, tropicamide
the action of atropine is ______
produce mydriasis, cycloplegia
mechanism of atropine is
antimuscarinic
the action of homatropine is ______
produce mydriasis, cycloplegia
mechanism of homatropine is
antimuscarinic
the action of tropicamide is
produce mydriasis, cycloplegia
mechanism of tropicamide is
antimuscarinic
ipatropium is used to treat
asthma, COPD
mechanism of ipatropium is
antimuscarinic
name an antimuscarinic used to treat asthma and COPD
ipatropium
neuromuscular blocking drugs
p. 304
neuromuscular blocking drugs are used for
muscle paralysis in surgery or mechanical ventilation
name a depolarising neurmuscular blocking drug
succinylcholine
name 6 nondepolarizing neuromuscular blocking drugs
tubocurarine
*mnemonic -- the "cur" drugs are nondepolarizing neuromuscular blocking agents
atracurium
is succinylcholine depolarizing or nondepolarizing?
depolarizing
is tubocurarine depolarizing or nondepolarizing?
nondepolarizing
is atracurium depolarizing or nondepolarizing?
nondepolarizing
is mivacurium depolarizing or nondepolarizing?
nondepolarizing
is pancuronium depolarizing or nondepolarizing?
nondepolarizing
is vacuronium depolarizing or nondepolarizing?
nondepolarizing
is rapacuronium depolarizing or nondepolarizing?
nondepolarizing
what is tubocurarine used for
nondepolarizing neuromuscular blockade
what agents are used to reverse neuromuscular blockade by succinylcholine?
cholinesterase inhibitors in phase II (ex -- neostigmine)
what phase of succinylcholine neuomuscular bloackade is reversible?
phase II (repolarized but blocked)
what agents are used to reverse pahse I neuromuscular blockade by succinylcholine?
phase I Succinylcholine neuromuscular blockade cannot be reversed
what phase of succinylcholine neuomuscular bloackade is irreversible?
phase I Succinylcholine neuromuscular blockade cannot be reversed
what is atracurium used for
nondepolarizing neuromuscular blockade
what is the effect of cholinesterase inhibitors on succinylcholine neuromuscular blockade?
phase I: cholinesterase inhibitors potentiates the blockade phase II: cholinesterase inhibitors reverse the blockade
what cholinesterase inhibitor is used to reverse phase II of succinylcholine neuromuscular blockade?
neostigmine
what is mivacurium used for
nondepolarizing neuromuscular blockade
Dantrolene
p. 304
what is dantrolene used for
treat malignant hyperthermia
what causes malignant hyperthermia
use inhalation anesthetics and succinylcholine together
what inhalation anesthetic DOES NOT cause malignanat hyperthermia?
N2O
what is dantrolene used for
neuroleptic malignant syndrome
what is neuroleptic malignant syndrome
a toxicity of antipsychotic drugs
what drug is used to treat malignant hyperthermia
dantrolene
what is the mechanism of dantrolene
prevents release of Ca++ from saarcoplasmic reticulum of skeletal muscle
Sympathomimetics
p. 305
epinephrine, NE, isoproterenol, dopamine, and dobutamine are all________________
catecholamines
catecholamines are_____________________
sympathomimetics
name 5 catecholamines
EPI, NE, Isoproterenol, dopamine, dobutamine
what receptors does epinephrine act on?
alpha-1, alpha-2, beta-1, beta-2 adrenergics
what receptors does NE work on?
alpha-1, alpha-2, beta-1 adrenergics
what receptors does isoproterenol work on?
beta-1 = beta-2 adrenergics
what receptors does dopamine work on?
D1 = D2, D1 and D2 more than beta, beta more than alpha
what receptors does dobutamine work on?
beta-1 > beta-2
which catecholamines are agonists to alpha-adrenergic receptors
EPI, NE > dopamine
which catecholamines are agonists to beta-1 adrenergic receptors
EPI, NE, Isoproterenol, dopamine, dobutamine
which catecholamines are agonists to beta-2 adrenergic receptors
EPI, isoproterenol, dopamine and dobutamine (less)
what is epinephrine used to treat?
anaphylaxis, open-angle glaucoma, asthma, hypotension
what is norepinephrine used to treat?
hypotension (but decreases renal perfusion)
what is isoproterenol used to treat?
AV block
what is dopamine used to treat
shock with renal failure, heart failure
what is dobutamine used to treat
shock, heart failure
what catecholamine is used to treat anaphylaxis
epinephrine ("EPI-pen")
what catecholamines are used to treat hypotension
EPI, NE
what catecholamine is used to treat asthma
epinephrine
what catecholamine is used to treat AV block
isoproterenol
what catecholamines are used to treat shock
doapmine, dobutamine
what is the action of amphetamine
indirect general adrenergic agonist, releases stored catecholamines
what is the action of ephedrine
indirect general adrenergic agonist, releases stored catecholamines
what is amphetamine used to treat
narcolepsy, obesity, attention deficit disorder
what is ephedrine used to treat
nasal decongestion, urinary incontinence, hypotension
name three sympathomimetic drugs used to treat hypotension
epinephrine, norepinephrin, ephedrine
what is the action of phenylephrine
adrenergic agonist, alpha-1 > alpha-2
what is the action of albuterol
adrenergic agonist, beta-2 >beta-1
what is the action of terbutaline
adrenergic agonist, beta-2 >beta-2
what is phenylephrine used for?
pupil dilator, vasoconstriction, nasal decongestion
what sympathomimetics are used to treat nasal congestion
ephedrine, phenylephrine
what is the mechanism of cocaine
indirect general adrenergic agonist, catecholamine uptake inhibitor
what is the action of cocaine
vasoconstriction, local anesthesia
what is the mechanism of clonidine
centrally acting alpha-adrenergic agonist, decreases central adrenergic outflow
what drug has the same mechanism as amphetamine
ephedrine
what is the mechanism of alpha-methyldopa
centrally acting alpha-adrenergic agonist, decreases central adrenergic outflow
what drug has the same mechanism as clonidine
alpha-methyldopa
what are clonidine and alpha-methyldopa used to treat
hypertension, especially in renal disease because they do not decreased blood flow to the kidney
what sympathomimetic is used to treat urinary incontinence
ephedrine
what sympathomimetic is used to treat attention deficit disorder
amphetamine
what sympathomimetic is used to treat narcolepsy
amphetamine
alpha-blockers
p. 306
name a nonselective irreversible alpha blocker
phenoxybenzamine
name a nonselective reversible alpha blocker
phentolamine
what is the mechanism of phenoxybenzamine
nonselective irreversible alpha blocker
what is the mechanism of phentolamine
nonselective reversible alpha blocker
what are phenoxybenzamine and phentolamine used for
pheochromocytoma
what are the side effects of nonselective alpha blockers
orthostatic hypotension, reflex tachycardia
name 3 alpha-1 selective adrenergic blockers
prazosin, terazosin, doxazosin
what is the mechanism of prazosin
alpha-1 selective adrenergic blocker
what is the mechanism of terazosin
alpha-1 selective adrenergic blocker
what is the mechanism of doxazosin
alpha-1 selective adrenergic blocker
what are alpha-1 selective adrenergic alpha blockers used for
hypertension, urinary retention in BPH
what are the side effects of alpha-1 blockers
orthostatic hypotension, dizziness, headache
what is prazosin used for?
hypertension, urinary retention in BPH
what drugs have the same action as prazosin
terazosin, doxazosin
what are the side effects of terazosin?
orthostatic hypotension, dizziness, headache
what selective alpha blockers cause orthostatic hypotension
phenoxybenzamine, phentolamine, terazosin, prazosin, doxazosin
name an alpha-2 selective adrenergic blocker
yohimbine
what is yohimbine used for
impotence (effectiveness controversial)
what alpha blockers are used to treat pheochromocytoma
phenoxybenzamine, phentolamine
beta-blockers ("lol"s)
p. 307
name some beta-blockers
propranolol, metoprolol, atenolol, nadolol, timolol, pindolol, esmolol, labetalol
what is the mechanism of propanolol
selective beta-adrenergic blocker
what is the mechanism of metoprolol
selective beta-adrenergic blocker
what is the mechanism of esmolol
selective beta-adrenergic blocker
what is the mechanism of pindolol
selective beta-adrenergic blocker
what are beta-blockers used to treat
hypertension, angina, MI, SVT, CHF, glaucoma
how do beta blockers treat hypertension
decrease cardiac output, decrease renin secretion
how do beta blockers treat angina
decrease heart rate, decrease cardiac contractility, decreased O2 consumption
why are beta blockers used to treat MI
decrease MI mortality
which beta blockers are used to treat SVT
propanolol, esmolol
how do propanolol and esmolol treat SVT
decrease AV conduction velocity
how do beta blockers treat CHF
slow progression of chronic failure
which beta blocker is used to treat glaucoma
timolol
what is timolol used to treat glaucoma
decrease secretion of aqueous humor
what are the toxic effects of beta blockers
impotence, exacerbation of asthma, caution in diabetes
what are the cardiovascular toxic effects of beta blockers
bradychardia, AV block, CHF
what are the CNS adverse effects of beta blockers
sedation, sleep alterations
which beta blockers are beta-1 selective
acebutolol, betaxolol, esmolol, atenolol, metaprolol (A BEAM of beta-1 blockers)
which beta-1 blocker is short-acting
esmolol
which beta blockers are non-selective
propanolol, timolol, pindolol, nadolol, labetalol
which beta blocker also blocks alpha receptors
labetalol (all others are spelled "olol")