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317 Cards in this Set

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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: Ach is synthesized from acetyl-CoA and choline by the enzyme ---------.
Choline acetyltransferase.
Autonomic drugs: The transport of choline into the nerve terminal can be inhibited by --------.
Hemicholinium.
Autonomic drugs: The release of transmitter from vesicles in the nerve ending require the entry of ------ into the neuron.
Calcium.
Autonomic drugs: --------- inhibits the release of the stored Ach.
Botulinum toxin.
Autonomic drugs: 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.
Noradrenergic:: Dopamine is transported into vesicles for hydroxylation to NE. This transport can be blocked by the drug --------.
Reserpine.
Noradrenergic:: The action of NE and DA is terminated by --------- and ----------.
Reuptake, diffusion (different than for Ach).
Noradrenergic:: --------- inhibits the release of the stored NE.
Guanethidine.
Noradrenergic:: The --------- drugs promote catecholamine release.
Amphetamine.
Noradrenergic:: The drugs --------- and ---------- inhibit the reuptake of NE.
Cocaine, TCA.
Noradrenergic:: The release of NE from a sympathetic nerve ending is modulated by ---------, --------- and ---------.
NE, Ach, angiotensin II.
Noradrenergic:: NE inhibits its own release at the noradrenergic nerve terminal through --------- receptors.
Alpha 2.
Noradrenergic:: Angiotensin II --------- (inhibits / stimulates) the release of NE from the noradrenergic nerve terminal.
Stimulates.
Noradrenergic:: Ach inhibits the release of NE from the noradrenergic nerve terminal by binding to --------- receptors.
M1.
What is the Clinical application and action of Bethanechol.
Postoperative and neurogenic ileus and urinary retention. / Activates bowel and bladder smooth muscle.
What are the Clinical application and action of Carbachol and Pilocarpine.
Glaucoma. / Activates ciliary muscle of eye (open angle), pupillary sphincter (narrow angle); Xerostomia assoc with Sjorgens Syndrome (Pilocarpine)
Clinical application / action of Neostigmine.
Indirect Ach Agonists/ anticholinesterase; Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative). / Increase endogenous Ach.
Clinical application / action of Pyridostigmine.
Indirect Ach Agonists/ anticholinesterase; Myasthenia gravis. / Increase Ach; increase strength.
Clinical application / action of Edrophonium.
Indirect Ach Agonists/ anticholinesterase;Diagnosis of myasthenia gravis (extremely short acting); differentiates between MG and cholinergic crisis/ Increase endogenous Ach.
Clinical application / action of Physostigmine.
Indirect Ach Agonists/ anticholinesterase; Glaucoma (crosses blood-brain barrier) and atropine overdose. / Increase endogenous Ach.
Clinical application / action of Echothiophate.
Indirect Ach Agonists/ anticholinesterase; Glaucoma. / Increase endogenous Ach; extremely long acting t1/2 = 100 hrs
What are the Symptoms of cholinesterase inhibitor poisoning.
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation (also abdominal cramping). "DUMBBELSS".
Indirect agonists (anticholinesterases):: Cholinesterase inhibitor poisoning may be caused by ---------.
Parathion and other organophosphates.
What is the clinical use for Donepezil and Tacrine?
Indirect Ach agonists used to treat Alzheimers dz
Indirect agonists (anticholinesterases):: Mechanism of action of Pralidoxime.
Regenerates active cholinesterase, chemical antagonist, used to treat organophosphate exposure. It acan be used as an antidote for cholinesterase inhibitor poisoning
Cholinoreceptor blockers:: 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."
Cholinoreceptor blockers:: 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."
Cholinoreceptor blockers:: Hexamethonium (ganglionic blocker) blocks -------- receptors.
Nicotinic.
What are some other drug categories with Anti Muscarinic activity?
Anti histamines Anti psychotics tricylic Anti depressants Anti arrythmics amantadine Meperedine
antimuscarinic drugs: "tropi" are anti-muscarinic
while vacationing in the tropics you lie on a beach and your muscles waste away!
antimuscarinic drugs: benztropine acts on the ____, and is used to treat
CNS, Parkinson's disease
antimuscarinic drugs: scopolamine acts on the _____, and is used to treat
CNS, motion sickness
What three antimuscarinics that act on eye and what is their MOA?
atropine, homatropine, tropicamide they all produce mydriasis and cyclopegia
what is the mechanism of ipatropium and what is it used to treat
its and antimuscarinic used to treat asthma, COPD
neuromuscular blocking drugs: neuromuscular blocking drugs are used for
muscle paralysis in surgery or mechanical ventilation
neuromuscular blocking drugs: name a depolarising neurmuscular blocking drug
succinylcholine
neuromuscular blocking drugs: name 6 nondepolarizing neuromuscular blocking drugs
tubocurarine
neuromuscular blocking drugs: *mnemonic -- the "cur" drugs are all _________ neuromuscular blocking agents
nondepolarizong
neuromuscular blocking drugs: what is tubocurarine used for
nondepolarizing neuromuscular blockade
neuromuscular blocking drugs: what agents are used to reverse neuromuscular blockade by succinylcholine?
cholinesterase inhibitors in phase II (ex -- neostigmine)
neuromuscular blocking drugs: what phase of succinylcholine neuomuscular bloackade is reversible?
phase II (repolarized but blocked)
neuromuscular blocking drugs: what agents are used to reverse pahse I neuromuscular blockade by succinylcholine?
phase I Succinylcholine neuromuscular blockade cannot be reversed
neuromuscular blocking drugs: what phase of succinylcholine neuomuscular bloackade is irreversible?
phase I Succinylcholine neuromuscular blockade cannot be reversed
neuromuscular blocking drugs: what is atracurium used for
nondepolarizing neuromuscular blockade
neuromuscular blocking drugs: 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
neuromuscular blocking drugs: what cholinesterase inhibitor is used to reverse phase II of succinylcholine neuromuscular blockade?
neostigmine
neuromuscular blocking drugs: what is mivacurium used for
nondepolarizing neuromuscular blockade
Dantrolene: what is dantrolene used for
treat malignant hyperthermia
Dantrolene: what causes malignant hyperthermia
use inhalation anesthetics and succinylcholine together
Dantrolene: what inhalation anesthetic DOES NOT cause malignanat hyperthermia?
N2O
Dantrolene: what is dantrolene used for
neuroleptic malignant syndrome
Dantrolene: what is neuroleptic malignant syndrome
a toxicity of antipsychotic drugs
Dantrolene: what drug is used to treat malignant hyperthermia
dantrolene
Dantrolene: what is the mechanism of dantrolene
prevents release of Ca++ from saarcoplasmic reticulum of skeletal muscle
Sympathomimetics: the 5 catecholamines
EPI, NE, Isoproterenol, dopamine, dobutamine
Sympathomimetics: what receptors does epinephrine act on and what is used for?
alpha-1, (alpha-2), beta-1, beta-2 adrenergics anaphylaxis, open-angle glaucoma, asthma, hypotension
Sympathomimetics: what receptors does NE work on and what is it used to treat?
alpha-1, (alpha-2), beta-1 adrenergics hypotension (but decreases renal perfusion)
Sympathomimetics: what receptors does isoproterenol work on and what is its clinical application?
beta-1 = beta-2 adrenergics AV block
Sympathomimetics: what receptors does dopamine work on and what is it used to treat?
D1 = D2, D1 and D2 more than beta, beta more than alpha shock with renal failure, heart failure
Sympathomimetics: what receptors does dobutamine work on and what is it used to treat?
beta-1 > beta-2 shock, heart failure
Sympathomimetics: what is the action of amphetamine and what are its clinical applications?
indirect general adrenergic agonist, releases stored catecholamines narcolepsy, obesity, attention deficit disorder
Sympathomimetics: what is the action of ephedrine and what are its clinical applications?
indirect general adrenergic agonist, releases stored catecholamines nasal decongestion, urinary incontinence, hypotension
Sympathomimetics: name three sympathomimetic drugs used to treat hypotension
epinephrine, norepinephrine, ephedrine
Sympathomimetics: what is the action of phenylephrine and what is it used for?
adrenergic agonist, alpha-1 > alpha-2 pupil dilator, vasoconstriction, nasal decongestion
Sympathomimetics: what is the action of albuterol and what is it used to treat?
adrenergic agonist, beta-2 >beta-1 asthma
Sympathomimetics: what is the action of terbutaline and what is it used to treat?
adrenergic agonist, beta-2 >beta-2 asthma
Sympathomimetics: what is the MOA of methoxamine and what is it used to treat?
alpha-1 paroxysmal atrial tachycardia, thru the vagal reflex
Sympathomimetics: what is the mechanism of cocaine and what are its actions?
indirect general adrenergic agonist, catecholamine uptake inhibitor it causes vasoconstriction, local anesthesia
Sympathomimetics: what is the mechanism of clonidine
centrally acting alpha-adrenergic agonist, decreases central adrenergic outflow
Sympathomimetics: what is the mechanism of alpha-methyldopa
centrally acting alpha-adrenergic agonist, decreases central adrenergic outflow
Sympathomimetics: what are clonidine and alpha-methyldopa used to treat
hypertension, especially in renal disease because they do not decreased blood flow to the kidney
Sympathomimetics: what sympathomimetic is used to treat urinary incontinence
ephedrine
Sympathomimetics: what sympathomimetic is used to treat attention deficit disorder and narcolepsy?
amphetamine
What is Epiniephrine Reversal?
use of an alpha 1 blocker to reverse HT to HYPOtension in a patient receiving too much epinephrine
alpha-blockers: what is the mechanism of phenoxybenzamine
nonselective irreversible alpha blocker
alpha-blockers: what is the mechanism of phentolamine
nonselective reversible alpha blocker
alpha-blockers: what are phenoxybenzamine and phentolamine used for?
pheochromocytoma
alpha-blockers: what are the side effects of nonselective alpha blockers
orthostatic hypotension, reflex tachycardia
alpha-blockers: name 3 alpha-1 selective adrenergic blockers
prazosin, terazosin, doxazosin the " -sin" drugs
alpha-blockers: what are alpha-1 selective adrenergic alpha blockers used for
hypertension, urinary retention in BPH
alpha-blockers: what are the side effects of alpha-1 blockers
first dose orthostatic hypotension, dizziness, headache
alpha-blockers: what are the side effects of terazosin?
orthostatic hypotension, dizziness, headache
alpha-blockers: what selective alpha blockers cause orthostatic hypotension
phenoxybenzamine, phentolamine, terazosin, prazosin, doxazosin
alpha-blockers: name an alpha-2 selective adrenergic blocker and what is it used for?
yohimbe
alpha-blockers: what is yohimbine used for
impotence (effectiveness controversial)
alpha-blockers: what alpha blockers are used to treat pheochromocytoma
phenoxybenzamine, phentolamine
What are some Pharmacological uses for Propanolol?
migraine prophylaxis, performance anxiety, essential tremor, Thryotoxicosis (blocks T3/T4 conversion; inhibits deiodinase activity)
beta-blockers ("lol"s): name some beta-blockers
propranolol, metoprolol, atenolol, nadolol, timolol, pindolol, esmolol, labetalol
beta-blockers ("lol"s): what are beta-blockers used to treat
hypertension, angina, MI, SVT, CHF, glaucoma
beta-blockers ("lol"s): how do beta blockers treat hypertension
decrease cardiac output, decrease renin secretion
beta-blockers ("lol"s): how do beta blockers treat angina
decrease heart rate, decrease cardiac contractility, decreased O2 consumption
beta-blockers ("lol"s): why are beta blockers used to treat MI
decrease MI mortality
beta-blockers ("lol"s): how do propanolol and esmolol treat SVT
decrease AV conduction velocity
beta-blockers ("lol"s): how do beta blockers used treat CHF
used to slow progression of chronic failure
beta-blockers ("lol"s): which beta blocker is used to treat glaucoma and how does it work?
timolol; decrease secretion of aqueous humor
beta-blockers ("lol"s): what are the toxic effects of beta blockers
impotence, exacerbation of asthma, CV adverse efx (bradycardia, AV block, CHF) CNS Adverse efx (sedation, sleep alterations); use with caution in diabetes b/c they block glycogenolysis and gluconeogenesis; some may INC LDLs, TGs
beta-blockers ("lol"s): what are the cardiovascular toxic effects of beta blockers
bradychardia, AV block, CHF
beta-blockers ("lol"s): what are the CNS adverse effects of beta blockers
sedation, sleep alterations
beta-blockers ("lol"s): which beta blockers are beta-1 selective
acebutolol, betaxolol, esmolol, atenolol, metaprolol (those that start with A-M)
beta-blockers ("lol"s): which beta-1 blocker is short-acting
esmolol
beta-blockers ("lol"s): which beta blockers are non-selective
propanolol, timolol, pindolol, nadolol, labetalol
beta-blockers ("lol"s): which beta blocker also blocks alpha receptors
labetalol (all others are spelled "olol")
What is Open Angle Glaucoma?
DEC reabsorption of aqueous humor causing an INC in IOP; P/W progressive PAINless visual loss; Treate with Beta blockers and Muscarinic activators
What is Closed Angle Glaucoma?
blockade of the canal of Schlemm causing an INC in IOP; Acutely PAINful; Tx with Cholinomimetics, Carbonic Anhydrase Inhibitors, and Mannitol
What drugs are CONTRAINDICATED in the Tx of CLOSED angle glaucoma?
Antimuscarinics, and alpha 1 agonists
How are Pilocarpine and Echothiophate used to treat Glaucoma and what are the Side Efx?
Closed Angle; INC the outflow of the AH; contract the ciliary muscle to open the trabecular meshwork; Side Efx miosis and cyclopegia
glaucoma drugs: what classes of drugs are used to treat glaucoma
alpha agonists, beta blockers, cholinomimetics, diuretics, prostaglandins (*mnemonic -- treating glaucoma is easy as ABCD)
glaucoma drugs: what is the effect of epinephrine in glaucoma
increase outflow of aqueous humor
glaucoma drugs: what are the side effects of epinephrine treatment in glaucoma
mydriasis, stinging
glaucoma drugs: what glaucoma should epinephrine NOT be used for
closed-angle glaucoma
glaucoma drugs: what is the effect of brimonidine in glaucoma
decreased aqueous humor synthesis
glaucoma drugs: what are the side effects of brimonidine treatment in glaucoma
no pupillary or vision changes
glaucoma drugs:What Beta blockers are used to treat Glaucoma and what is the effect?
Timolol, (betaxolol, carteolol); decrease aqueous humor secretion
glaucoma drugs: what is the effect of cholinomimetics in glaucoma
ciliary muscle contraction, opening of trabecular meshwork, increase outflow of aqueous humor
glaucoma drugs: what is the effect of diuretic treatment in glaucoma
inhibition of carbonic anhydrase --> decrease HCO3 secretion --> decrease aqueous humor secretion
glaucoma drugs: what is the effect of prostaglandin (latanoprost) treatment in glaucoma and what are the Side Efx?
increase outflow of aqueous humor; darkens color of iris (browning)
glaucoma drugs: which drugs used to treat glaucoma increase outflow of aqueous humor
cholinomimetics, prostaglandin, epinephrine
glaucoma drugs: which glaucoma drugs decrease aqueous secretion
beta blockers, diuretics
L-dopa/carbidopa: what is the mechanism of action of L-dopa/carbidopa and what are they used to treat?
increase dopamine level in brain; Parkinson's disease
L-dopa/carbidopa: how does L-dopa differ from dopamine?
L-dopa can cross the blood-brain barrier, dopamine cannot
L-dopa/carbidopa: what happens to L-dopa after it crosses the BBB
converted to dopamine by dopa decarboxylase
L-dopa/carbidopa: what enzyme convertes L-dopa to dopamine
dopa decarboxylase
L-dopa/carbidopa: what is the function of carbidopa
peripheral decarboxylase inhibitor
L-dopa/carbidopa: why is carbidopa given with L-dopa
increase L-dopa availability in CNS by inhibiting decarboxylase in periphery, also limits peripheral side effects
L-dopa/carbidopa: what are the side effects of L-dopa.carbidopa treatment
arrhythmias due to peripheral efx, dyskinesias due to excess dopamine stimulation
Parkinson's disease drugs: what classes of drugs are used to treat Parkinson's disease
dopamine agonists, MAO inhibitors, antimuscarinics
Parkinson's disease drugs: specifically, which drugs are used to treat Parkinson's
Bromocriptine, Amantadine, Levodopa, Selegiline, Antimuscarinics (BALSA)
Parkinson's disease drugs: which dopamine agosts are used to treat Parkinson's
L-dopa/carbidopa, bromocriptine, pramipexole, ropinirole, amantadine
Parkinson's disease drugs: what is the action of bromocriptine in Parkinson's
ergot alkaloid, partial dopamine agonist
Parkinson's disease drugs: what is the action of amantadine in Parkinson's
enhances dopamine release
Parkinson's disease drugs: what is the mechanism of selegiline
selective MAO type B inhibitor
Parkinson's disease drugs: what is the effect of benztropine in Parkinson's
improves tremor, rigidity, little effect on bradykinesia
Sumatriptan: what is its MOA and what is it used for?
5-HT1D agonist; acute migraine, cluster headache attacks
Sumatriptan: what is the half life of sumatriptan, what are some Side Efx?
less than 2 hours; chest discomfort, mild tingling
Sumatriptan: what are the contraindications for sumatriptan
patients with CAD or Prinzmetal's angina
Epilepsy drugs: which drugs are used for simple and complex partial seizures
phenytoin, carbamazapine, lamotrigine, gabapentin, topiramate, phenobarbital
Epilepsy drugs: what types of seizures is phenytoin indicated for
simple and complex partial, tonic-clonic, status epilepticus
Epilepsy drugs: what types of seizures is carbamazepine indicated for
simple and complex partial, tonic-clonic
Epilepsy drugs: what types of seizures is lamotrigine indicated for
simple and complex partial, tonic-clonic
Epilepsy drugs: what types of seizures is gabapentin indicated for
simple and complex partial, tonic-clonic
Epilepsy drugs: what types of seizures is topiramate indicated for
simple and complex partial
Epilepsy drugs: what types of seizures is phenobarbital indicated for
simple and complex partial, tonic-clonic
Epilepsy drugs: what drugs can be used for tonic-clonic seizures
phenytoin, carbamazapine, lamotrigine, gabapentin, phenobarbital, valproate
Epilepsy drugs: what drugs can be used for absence seizures
valproate, ethosuximide
Epilepsy drugs: what drugs can be used for status epilepticus
phenytoin, benzodiazapines (diazepam, lorazepam)
Epilepsy drugs: what types of seizure is valproate indicated for
tonic-clonic, absence
Epilepsy drugs: what types of seizure is ethosuximide inidcated for
absence
Epilepsy drugs: what type of seizure are benzodiazepines indicated for
status epilepticus
Epilepsy drugs: other than anti-seizure, what else is phenytoin used for
class 1B anti-arrhythmic
Epilepsy drugs: how should a patient taking carbamazepine be followed
monitor LFT's weekly
Epilepsy drugs: which seizure drugs have adjunct use
gabapentin, topiramate
Epilepsy drugs: which seizure drug is safest in pregnant women
phenobarbital
Epilepsy drugs: which seizure drug is used in Crigler-Najjar II
phenobarbital
Epilepsy drugs: what are the advantages of phenobarbital
can be used in pregnant women, Crigler Najjar II
Epilepsy drug toxicities: what are the side effects of benzodiazepines
sedation, tolerance, dependence
Epilepsy drug toxicities: what are the side effects of carbamazepine
diplopia, ataxia, CYP induction, blood dyscrasias, liver toxicity
Epilepsy drug toxicities: what are the side effects of ethosuximide
GI distress, lethargy, headache, urticaria, Stevens-Johnson syndrome
Epilepsy drug toxicities: what are the side effects of phenobarbital
sedation, CYP induction, tolerance, dependence
Epilepsy drug toxicities: what are the side effects of phenytoin
nystagmus, diplopia, ataxia, sedation, ginigival hyperplasia, hirsutism, anemias, teratogenic
Epilepsy drug toxicities: what are the side effects of valproate
GI distress, rare by fatal hepatotoxicity, neural tube defects (spina bifida)
Epilepsy drug toxicities: what are the side effects of lamotrigine
life-threatening rash, Stevens-Johnson syndrome
Epilepsy drug toxicities: what are the side effects of gabapentin
sedation, movement disorders
Epilepsy drug toxicities: what are the side effects of topiramate
sedation, mental dulling, kidney stones, weight loss
Epilepsy drug toxicities: which anti-epileptic drug is teratogenic
phenytoin
Epilepsy drug toxicities: which anti-epileptic drug can cause dependence
benzodiazepines, phenobarbital
Epilepsy drug toxicities: which anti-epileptic drug can cause neural tube defects
valproate
Epilepsy drug toxicities: which anti-epileptic drugs can cause GI distress
valproate, ethosuximide
Epilepsy drug toxicities: it is necessary to check LFT's with which anti-epileptic drugs
carbamazepine, valproate
Epilepsy drug toxicities: which anti-epileptic drugs cause CYP induction
phenobarbital, carbamazepine
Epilepsy drug toxicities: which anti-epileptic drugs can cause blood problems
carbamazepine, phenytoin
Epilepsy drug toxicities: which anti-epileptic drugs can cause Stevens-Johnson syndrome
lamotrigine, ethosuximide
Epilepsy drug toxicities: which anti-epileptic drugs can cause diplopia
carbamazepine, phenytoin
Phenytoin: what is the mechanism of phenytoin action
use-dependent blockade of Na+ channels
Phenytoin: what is the clinical application of phenytoin
grand mal seizures
Phenytoin: what are the toxicities of phenytoin
nystagmus, ataxia, diplopia, lethargy
Phenytoin: what are the chronic toxicities of phenytoin
gingival hyperplasia in children, peripheral neuropathy, hirsutism, megaloblastic anemia, malignant hyperthermia (rare)
Phenytoin: should pregnant women take phenytoin
NO -- teratogenic
Phenytoin: why does phenytoin cause megaloblastic anemia
causes decreased vitamin B-12
Barbiturates: name 4 barbiturates
phenobarbital, pentobarbital, thiopental, secobarbital
Barbiturates: what is the mechanism of barbiturate action
increase duration of Cl channel opening --> decreased neuron firing --> facilitate GABA-A action
Barbiturates: how do barbiturates facilitate GABA-A action
increase duration of Cl channel opening which decreases neuron firing (Barbidurate increases duration
Barbiturates: is barbiturate action on the CNS stimulatory or inhibitory
inhibitory
Barbiturates: what is the clinical application of barbiturates
sedative for anxiety, seizures, insomnia, anesthesia induction (thiopental)
Barbiturates: which barbiturate is used for anesthesia induction
thiopental
Barbiturates: what are the side effects of barbiturates
dependence, additive CNS depression effects with alcohol, respiratory or CV depression (death), drug interactions due to CYP induction
Barbiturates: what should you find out before giving a patient barbiturates
what other medications they take, because of CYP induction and many drug interactions
Barbiturates: what happens if you give barbiturates to a patient in alcohol-induced coma or DT's
they might DIE!! Because of additive effect of barbiturates and alcohol --> respiratory depression
Barbiturates: when are barbiturates contra-indicated
porphyria
Barbiturates: can barbiturates cause dependence
YES
Barbiturates: My friend Barb was very anxious so her doctor gave her barbiturates to increase the duration of the time she could speak in public without freaking out and having a seizure. She became so dependent on it that she recommended it to her friend Portia who couldn't take it because of porphyria. One day Barb drank too much alcohol and took her barbiturates and never woke up! THE END
clinical pharmacology made ridiculous. Period
Benzodiazepines: name a bunch of benzodiazepines
diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide (all have ZZZ in them)
Benzodiazepines: what is the mechanism of benzodiazepines
increase frequency of Cl channel opening --> facilitate GABA-A action (Frenzodiazepines increase frequency)
Benzodiazepines: which GABA receptors are facilitated by barbiturates and bezodiazepines
GABA-A
Benzodiazepines: what are the clinical applications of benzodiazepines
anxiety, spasticity, status epilepticus (diazepam), detoxification (alcohol withdrawal, DT's)
Benzodiazepines: which benzodiazepine can be used for status epilepticus
diazepam
Benzodiazepines: what drugs can be used to treat alcohol withdrawal
benzodiazepines
Benzodiazepines: which benzodiazepines are short-acting
TOM thumb: Triazolam, Oxazepam, Midazolam
Benzodiazepines: what are the toxic effects of benzos
dependence, additive CNS depression effects with alcohol
Benzodiazepines: how are benzos better than barbiturates
less respiratory depression and coma risk
Benzodiazepines: how do you treat benzo overdose
flumazenil
Benzodiazepines: what is flumzenil used for
benzo overdose
Benzodiazepines: how does flumazenil work
competitive antagonist at GABA receptor
Benzodiazepines: can a patient become benzodiazepine dependent
YES
Benzodiazepines: are barbiturates or benzodiazepines used for alcohol withdrawal
benzodiazepines
Antipsychotics (neuroleptics): what is another name for antipsychotics
neuroleptics
Antipsychotics (neuroleptics): name 4 antipsychotic drugs
thioridazine, haloperidol, fluphenazine, chlorpromazine
Antipsychotics (neuroleptics): how do you keep benzos straight from antipsychotics
Benzos help 3rd year Jon Kazam be less anxious around patients: Shazam Kazam! Without antipsychotics patients talk like a crazy 'zine (well, not perfect, but I'm working on it)
Antipsychotics (neuroleptics): what is the mechanism of most antipsychotics
block dopamine D2 receptors
Antipsychotics (neuroleptics): what is the clinical application of antipsychotics
schizophrenia, psychosis
Antipsychotics (neuroleptics): what are the side effects of antipsychotics
extrapyramidal side effects (EPS), sedation, endocrine, muscarinic blockade, alpha blockade, histamine blockade
Antipsychotics (neuroleptics): what is a long-term effect of antipsychotic use
tardive dyskinesia
Antipsychotics (neuroleptics): what is neuroleptic malignant syndrome
a side effect of antipsychotics; rigidity, autonomic instability, hyperpyrexia
Antipsychotics (neuroleptics): how do you treat neuroleptic malignant syndrome
dantrolene, dopamine agonists
Antipsychotics (neuroleptics): what is tardive dyskinesia
side effect of neuroleptics; stereotypic oral-facial movements, may be due to dopamine receptor sensitization
Antipsychotics (neuroleptics): what is the "rule of 4" with EPS side effects from antipsychotic drugs
evolution of EPS side effects: 4 hours -- acite dystonia, 4 days -- akinesia, 4 weeks -- akasthesia, 4 months -- tardvie dyskinesia
Antipsychotics (neuroleptics): is tardvie dyskinesia reversible
often irreversible
Antipsychotics (neuroleptics): what is fluphenazine used for
schizophrenia, psychosis
Atypical antipsychotics: name 3 atypical antipsychotics
clozapine, olanzapine, risperidone
Atypical antipsychotics: what type of antipsychotic is clozapine
atypical
Atypical antipsychotics: what type of antipsychotic is olanzapine
atypical
Atypical antipsychotics: what type of antipsychotic is risperidone
atypical
Atypical antipsychotics: what is the mechanism of atypical antipsychotics
block 5-HT2 and dopamine receptors
Atypical antipsychotics: what is the mechanism of clozapine
block 5-HT2 and dopamine receptors
Atypical antipsychotics: what is the mechanism of olanzapine
block 5-HT2 and dopamine receptors
Atypical antipsychotics: what is the mechanism of risperidone
block 5-HT2 and dopamine receptors
Atypical antipsychotics: what is the clinical application of clozapine
schizophrenia positive and negative symptoms
Atypical antipsychotics: what is the clinical application of olanzapine
schizophrenia positive and negative symptoms, OCD, anxiety disorder, depression
Atypical antipsychotics: what is the clinical application of risperidone
schizophrenia positive and negative symptoms
Atypical antipsychotics: how are atypical antipsychotics different from classic ones
atypicals treat positive and negative symptoms of schizophrenia, fewer extrapyramidal and anticholinergic side effects than classic antipsychotics
Atypical antipsychotics: which antipsychotics should be used to treat positive and negative symptoms of schizophrenia
atypical ones -- clozapine, olanzapine, risperidone
Atypical antipsychotics: which antipsychotics should be used for fewer side effects
atypical ones -- clozapine, olanzapine, risperidone
Atypical antipsychotics: what is a potential toxicity of clozapine
agranulocytosis
Atypical antipsychotics: which antipsychotic drug can cause agranulocytosis
clozapine
Atypical antipsychotics: what test must be done weekly on patients taking clozapine
WBC count because of potential agranulocytosis
Lithium: what is the mechanism of action of lithium
unknown; may be related to inhibition of phosphoinositol cascade
Lithium: what is the clinical application of lithium
mood stabilizer for bipolar disorder
Lithium: how does lithium help people with bipolar disorder
prevents relapse and acute manic episodes
Lithium: what are the side effects of lithium
tremor, hypothyroidism, polyuria, teratogenic
Lithium: is it OK for women taking lithium to get pregnant
NO -- teratogenic
Lithium: what does lithium cause polyuria
ADH antagonist --> nephrogenic diabetes insipidus
Lithium: AUTHOR
Hina Talib
Antidepressants: What do the following drugs inhibit: 1. MAO inhibitors, 2. Desipramine/maprotilline, 3. Mirtazapine and 4. Fluoxetine/trazodone?
1. MAO 2. NE reuptake 3. Alpha 2-R 4. 5HT reuptake
Antidepressants: All of the above actions are ------synaptic
PRE
List the Tricyclic Antidepressants: What are the three C's of their toxicity?
Convulsions, Coma, Cardiotoxicity (arrythmias). Also respiratory depression, hypyrexia.
List the Tricyclic Antidepressants: How about toxicity in the eldery?
confusion and hallucinations due to anticholinergic SE
List the Tricyclic Antidepressants: What is the mechanism of TCA?
block reuptake of NE and 5HT
List the Tricyclic Antidepressants: What is the clinical uses of TCAs?
Endogenous depresion. Bed wetting - imipramine. OCD- clomipramine.
List the Tricyclic Antidepressants: How are tertiary TCA's different than secondary in terms of side effects?
Amitriptyline (tertiary) has more anti-cholinergic effects than do secondary (nortriptyline). Desipramine is the least sedating.
List the Tricyclic Antidepressants: what are the SE of TCAs?
sedation, alpha blocking effects, atropine-like anti cholinergic side effects (tachycardia, urinary retention)
List the Tricyclic Antidepressants: Fluoxetine, sertraline, paroxetine, citalopram are what class of drugs?
pg 311 SSRI's for endogenous depression
List the Tricyclic Antidepressants: How long does it take an anti-depressant to have an effect?
2-3weeks
List the Tricyclic Antidepressants: How does the toxicity differ fromTCA's and what are they?
Fewer than TCA's. CNS stimulation - anxiety, insomnia, tremor, anorexia, nausea, and vomiting.
List the Tricyclic Antidepressants: What toxicity happens with SSRI's and MAO inhibitors given together?
Seratonin Syndrome! Hyperthermia, muscle rigidity, cardiovascular collapse
List the Tricyclic Antidepressants: What are heterocyclics?
pg 312 2nd and 3rd generation antidepressants with varied and mixed mechanisms of action. Used major depression.
List the Tricyclic Antidepressants: Examples of heterocyclics?
trazodone, buproprion, venlafaxine, mirtazapine, maprotiline
List the Tricyclic Antidepressants: Which one is used for smoking cessation?
Buproprion. Mechanism not known. Toxicity - stimulant effects, dry mouth, aggrevation of pyschosis
List the Tricyclic Antidepressants: Which one used in GAD?
Venlafaxine - inhibits 5HT and DA reuptake. Toxicity - stimulant effects
List the Tricyclic Antidepressants: which one blocks NE reuptake
maprotiline
List the Tricyclic Antidepressants: Which one increases release of NE and 5HT via alpha 2 antagonism?
mirtazapine. Also potent 5HT Rantagonist. Toxicity - sedation, increase serum cholesterol, increase apetite
List the Tricyclic Antidepressants: What is trazodone and it' SE?
primarily inhibits seratonin reuptake. Toxicity - sedation, nausea, priapism, postural hypotension
Give 2 examples of MAO: Mechanism and Clinical Uses?
non selevtive MAO inhibition. Atypical antidepressant, anxiety, hypochondriasis
Give 2 examples of MAO: What is the toxicity with tyramine ingestion (in foods) and meperidine?
Hypertensive crisis
Give 2 examples of MAO: Other toxicities?
CNS stimulation, contraindicated with SSRI's or B-agonists
What is the mechanims of selgiline (deprenyl)?: what is the clinical use and toxicity?
adjunctive agent to L-dopa for Parkinsons. May enhance adverse effects of L-dopa
General principles: What is the significance of drugs with decreased solubility in blood?
rapid induction and recovery times . Ie. N20
General principles: What is the significance of drugs with increased solubility in blood?
increased potency = I/ MAC. Ie. Halothane
Inhaled Anesthetics: list them
halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide
Inhaled Anesthetics: What is good about lower solubility?
the quicker the anesthetic response, and the quicker the recovery
Inhaled Anesthetics: What are these drug's effects?
myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow
Inhaled Anesthetics: What toxicity mactches the following drugs 1. Halothane 2. Methoxyflurane 3. Enflurane 4. Rare
1. Hepatotoxcity 2. Nephrotoxicty 3. Proconvulsant 4. Malignant hyperthermia
IV anesthetics: What do barbituates, benzodiazepines, arylcyclohexylamines and narcotic analgesics have in common?
they are IV anesthetics
IV anesthetics: What the pharmacokinetics and uses of thiopental?
high lipid solubility, rapid entry into brain. Used for induction of anesthesia for short surgical procedures. Terminated by redistribution from brain. Decreased cerebral blood flow
IV anesthetics: Give an example of a benzo and what is this class's shortcoming?
midazolam used for endoscopy. Used with gaseous anesthetics and narcotics. May cause severe post-op respiratory depressio and amnesia
IV anesthetics: What does Ketamine (PCP analog and an arylcyclohexylamine) do?
dissociative anesthetic. Cardiovascular stimulant. Causes disorientation, hallucination, bad dreams. Increases cerebral blood flow.
IV anesthetics: How are narcotic analgesics used? Examples?
Morphone and fentanyl are used with CNS depressant during general anesthesia.
IV anesthetics: What is the advantage of propofol
used for rapid anesthesia induction and short procedures. Less post-op nausea than thiopental
Local anesthetics: Name some esters?
procaine, cocaine, tetracaine,
Local anesthetics: Name some amides?
lidocaine, bupivacaine, (amides have two I's in name!)
Local anesthetics: What is the mechanism and clinical use?
bind receptor and block Na channels. Tertiary amine local anesthetics penetrate membrane in uncharge form, then bind charged form. Use for minor surgical procedures, spinal anesthesia.
Local anesthetics: How do you decide to use ester or amides?
if allergic to esters, give amides
Local anesthetics: what is the toxicity
CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, arrhythmias (cocaine)
Local anesthetics: In infected ________ tissue, anesthetics are charged and cannot penetrate membrane. Therefore, ______ anesthetics are needed.
acidic; more
Local anesthetics: What is the order of nerve blockade for size and myelination? Which factor predominates?
small diameter> large diameter. Myelinated fibers> unmyelinated fibers. Size factor predominates
Local anesthetics: what is the order of loss of sensation?
pain first, then temp, then touch, then pressure
Local anesthetics: Why would you give these drugs with vasoconstrictors?
to enhance local action
Opiod analgesics: List as many as you can.
morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan
Opiod analgesics: Mechanism: They act as _____ for opiod receptors to modulate synaptic transmission
agonists
Opiod analgesics: which drugs act at the mu, delta, kappa receptors?
morphine enkephalin, dynorphin
Opiod analgesics: Clinical use?
pain, cough supression (dex), diarrhea (loperamide), acute pulmonary edema, methadone maintenance programs
Opiod analgesics: What are the major toxicities?
addiction, respiratory depression, constipation, miosis, additive CNS depression wth other drugs
Opiod analgesics: Tolerance does not develop to __________and ______
miosis and constipation
Opiod analgesics: How would you treat toxicity?
naloxone, naltrexone (opiod R antagonist)
Other NSAIDS: List three NSAIDS?
ibuprofen, naproxen, indomethacin
Other NSAIDS: What is their mechanism?
reversibly inhibit COX 1 and 2. Blocks PG synthesis
Other NSAIDS: What is their clinical use (3As)?
Antipyretic, analgesic, anti-inflammatory. Indomethacin is used to close a PDA.
Other NSAIDS: What are common toxicities?
renal damage, aplastic anemia, GI distress, ulcers
COX 2 Inhibitors: Where is cox2 found?
in inflammatory cells and mediates inflammation and pain
COX 2 Inhibitors: Why is cox2 inhibition better than cox1?
cox1 helps to maintain gastric mucosa, thus, should not have the corrosive effects of other NSAIDs on the GI lining (less incidence of ulcers and bleeding)
COX 2 Inhibitors: Clinical Use?
RA and osteoarthritis
Acetaminophen: What is its mechanism and where does it work?
reversibly inhibits cox, mostly in CNS. Inactivated peripherally.
Acetaminophen: What are its 2 As?
antipyretic, analgesic but NOT anti-inflammatory.
Acetaminophen: Overdose effects?
hepatic necrosis, acetaminophen metabolites depletes glutathine and forms toxic tissue adducts in the liver