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Pharmacology
Review for Pharmacology Exam
436
Pharmacology
Professional
10/08/2015

Additional Pharmacology Flashcards

 


 

Cards

Term
List two clinical uses of norepinephrine.
Definition
Hypotension, pressor agent.
Term
What receptors does norepinephrine primarily bind to?
Definition
alpha/beta 1, beta 3.
Term
Does norepinephrine circulate?
Definition
No. It is released by neurons.
Term
List two types of drugs that interact with norepinephrine.
Definition
Monoamine oxidase inhibitors and tricyclic antidepressants.
Term
What is the drug of choice for allergic reactions?
Definition
Epinephrine.
Term
What receptors does epinephrine interact with?
Definition
Alpha/beta 1, beta 2.
Term
Does epinephrine circulate?
Definition
Yes. It is released by the adrenal medulla into the circulation.
Term
List two classes of drugs that epinephrine interacts with.
Definition
Monoamine oxidase inhibitors and tricyclic antidepressants.
Term
What is the drug of choice for shock?
Definition
Norepinephrine (dopamine is a close second).
Term
What receptors does dopamine bind to?
Definition
Alpha-1, beta-1, and D.
Term
What drug is a precursor for norepinephrine?
Definition
Dopamine.
Term
What class of drug interacts with dopamine?
Definition
Monoamine oxidase inhibitors.
Term
List two uses of isoproterenol.
Definition
Asthma, cardiac stimulant.
Term
What receptors does isoproterenol interact with?
Definition
Beta.
Term
Is isoproterenol synthetic or endogenous?
Definition
Synthetic.
Term
What is the effect of isoproterenol on blood pressure and heart rate?
Definition
Isoproterenol decreases blood pressure and increases heart rate.
Term
List two uses of phenylephrine.
Definition
Nasal decongestant and hypotension.
Term
What is the receptor that phenylephrine binds to?
Definition
Alpha-1 (agonist).
Term
What is a side effect of phenylephrine?
Definition
Reflex bradycardia.
Term
What is methoxamine used for?
Definition
Hypotension, pressor agent (not commonly used).
Term
What receptor does methoxamine bind to?
Definition
Alpha-1 (agonist).
Term
What is a side effect of methoxamine?
Definition
Reflex bradycardia.
Term
What is clonidine used for?
Definition
Hypertension.
Term
What receptor does clonidine bind to, and is it an agonist or an antagonist?
Definition
Alpha-2 agonist.
Term
What is the mechanism of clonidine action?
Definition
It is an alpha-2 agonist that decreases CNS sympathetic outflow and inhibits the release of norepinephrine.
Term
What is a major risk in discontinuing clonidine use?
Definition
Rebound hypertension.
Term
What are three side effects of clonidine?
Definition
Dry mouth, sedation, impotence.
Term
What is alpha-methyldopa used for?
Definition
Hypertension.
Term
What is the mechanism of action of alpha-methyldopa?
Definition
It binds to alpha-2 receptors and decreases CNS sympathetic output and norepinephrine release.
Term
What is a risk of discontinuing alpha-methyldopa use?
Definition
Rebound hypertension.
Term
List 3 side effects of alpha-methyldopa.
Definition
Dry mouth, sedation, impotence.
Term
What is alpha-methyldopa metabolized to?
Definition
Alpha-methylnorepinephrine.
Term
What are two uses of dobutamine?
Definition
Congestive heart failure and cardiac stimulant.
Term
What is the mechanism of dobutamine?
Definition
It is a beta-1 agonist that increases force of contraction without increasing heart rate or oxygen demand.
Term
List two problems with dobutamine.
Definition
Tolerance and desensitization.
Term
What is albuterol used for?
Definition
Asthma, bronchodilator.
Term
What receptor is albuterol selective for?
Definition
It is beta-2 selective (agonist).
Term
What is the onset and duration if albuterol is administered orally?
Definition
1-2 hours to onset and 4-6 hour duration.
Term
What is the onset and duration of albuterol if administered by inhalation?
Definition
5-10 minute onset and 3-4 hour duration.
Term
What type of side effects can occur with albuterol use?
Definition
Cardiovascular (less with inhalation).
Term
What is ritodrine used for?
Definition
Premature labor.
Term
What is ritodrine's mechanism.
Definition
Beta-2 agonist.
Term
Explain how mydriasis occurs.
Definition
Activation of alpha-1 receptors on the radial muscle causes pupil dilation.
Term
Explain how miosis occurs.
Definition
Activation of M2 and M3 receptors on the circular muscle by the parasympathetic nervous system causes contraction of the circular muscle and pupil constriction.
Term
Explain how accommodation occurs.
Definition
Activation of M3 receptors on the ciliary muscle causes contraction.
Term
Explain the receptor involved and the response to sympathetic stimulation of the heart.
Definition
Activation of the beta-1 receptor causes increased heart rate and force of contraction.
Term
Explain how the parasympathetic nervous system acts on the heart.
Definition
Activation of M2 receptors causes a decrease in heart rate.
Term
Explain how the sympathetic nervous system acts on the vascular muscle.
Definition
Activation of alpha-1 receptors causes constriction. Activation of beta-2 receptors causes relaxation.
Term
Explain how the parasympathetic nervous system acts on vascular muscle.
Definition
NO causes relaxation (M3 receptor involved).
Term
Explain how the sympathetic nervous system acts on bronchial muscle.
Definition
Activation of beta-2 receptors causes relaxation.
Term
Explain how the parasympathetic nervous system acts on bronchial muscle.
Definition
Activation of M receptors causes contraction.
Term
Explain how the sympathetic nervous system acts on the GI tract.
Definition
Activation of the alpha-1 and beta-2 receptors decreases motility.
Term
Explain how the parasympathetic nervous system acts on the GI tract.
Definition
Activation of M3 receptors causes increased motility.
Term
Explain how the sympathetic nervous system acts on genitourinary muscle.
Definition
Activation of beta-2 receptors causes relaxation.
Term
Explain how the parasympathetic nervous system acts on genitourinary muscle.
Definition
Activation of M3 receptors causes contraction.
Term
Explain how the sympathetic nervous system acts on the uterus.
Definition
Activation of beta-2 receptors causes relaxation.
Term
Explain how the sympathetic nervous system acts on the pilomotor muscles.
Definition
Activation of alpha receptors causes contraction.
Term
Explain how the sympathetic nervous system acts on the sweat glands.
Definition
Activation of M3 receptors causes increased secretion.
Term
Explain how the sympathetic nervous system acts on the liver.
Definition
Activation of beta-2 receptors causes release of glucose.
Term
Explain how the sympathetic nervous system acts on the kidney.
Definition
Activation of beta-1 receptors increases renin.
Term
Explain how the sympathetic nervous system acts on fat cells.
Definition
Activation of beta-3 receptors stimulates lipolysis.
Term
What second messenger is produced upon activation of beta receptors and D1 and D5 receptors?
Definition
cAMP.
Term
What second messenger is produced upon activation of alpha-1 receptors and M1, M3, and M5 receptors?
Definition
IP3/Ca2+
Term
What second messenger is affected by stimulation of alpha-2, M2, M4, D2,D3, and D4 receptors?
Definition
cAMP decreases.
Term
What ion flow occurs as a result of activation of nicotinic receptors?
Definition
Sodium in, potassium out.
Term
What is the formula for blood pressure?
Definition
BP = CO x TPR
Term
What is the formula for cardiac output?
Definition
CO = SV x HR
Term
What does the baroreceptor reflex respond to?
Definition
Blood pressure change (not heart rate change).
Term
What is the effect of alpha-1 receptor activation on total peripheral resistance and blood pressure?
Definition
Increased TPR, increased BP.
Term
What is the effect of beta-1 receptor activation on heart rate, cardiac output, and blood pressure?
Definition
Increase.
Term
What is the effect of beta-2 receptor activation on total peripheral resistance and blood pressure?
Definition
Decrease.
Term
What is the effect of M2 receptor activation on heart rate, cardiac output, and blood pressure?
Definition
Decrease.
Term
What is the effect of M3 receptor activation on total peripheral resistance and blood pressure?
Definition
Decrease.
Term
Are vascular beta-2 and M3 receptors innervated?
Definition
No.
Term
What is the effect of norepinephrine on heart rate and blood pressure?
Definition
Decreased heart rate and increased blood pressure.
Term
What is the effect of isoproterenol on blood pressure, heart rate, and PP?
Definition
BP (o/-), increased heart rate, increased PP.
Term
What is the effect of epinephrine on BP, HR, and PP?
Definition
Increase.
Term
What is the effect of mecamylamine on blood pressure and heart rate?
Definition
Decreased blood pressure and (0/+) HR.
Term
What is the effect of propranolol on blood pressure and heart rate?
Definition
BP (0/-), decreased heart rate.
Term
What is the effect of atropine on blood pressure and heart rate?
Definition
BP (0/-), increased heart rate.
Term
What is the effect of phentolamine on blood pressure, heart rate, and PP?
Definition
Decreased blood pressure, increased heart rate, increased PP.
Term
Epinephrine counters the effects of the physiological release of what molecule?
Definition
Histamine.
Term
What is the effect of norepinephrine on renal vasculature?
Definition
Vasoconstriction.
Term
What is the effect of dopamine on renal vasculature?
Definition
Vasodilation.
Term
List two drugs of choice/frontline agents for chronic glaucoma.
Definition
Timolol and latanoprost.
Term
What is the mechanism of action of timolol?
Definition
It is a beta-blocker that helps glaucoma by decreasing secretion.
Term
What is the mechanism of action of latanoprost?
Definition
Latanoprost is a PGF2alpha analogue that treats chronic glaucoma by increasing outflow.
Term
What are 3 side effects of latanoprost?
Definition
Red eye, long eyelashes, and dark pupils.
Term
List four frontline agents for hypertensive crisis.
Definition
Alpha-blockers, labetalol, carvedilol, and fenoldopam.
Term
What is the mechanism of action of labetalol and carvedilol?
Definition
Alpha/beta blockers reduce blood pressure and heart rate.
Term
Give two examples of alpha-blockers.
Definition
Phenoxybenzamine and phentolamine.
Term
What is the mechanism of action of Fenoldopam?
Definition
D1a-agonist used for acute hypertension and renal failure.
Term
Which beta-blockers are beta-1 selective?
Definition
A-M
Term
List three contraindications for use of beta-blockers.
Definition
Unstable CHF, asthma, and diabetes.
Term
What is the front-line agent for emergency glaucoma treatment?
Definition
Pilocarpine.
Term
What is the mechanism of action of pilocarpine?
Definition
M-agonist increases outflow.
Term
What is the front-line agent for reversing atropine toxicity?
Definition
Physostigmine.
Term
What is the mechanism of action of physostigmine?
Definition
It is a reversible acetylcholinesterase inhibitor that can cross the BBB.
Term
What is the front-line agent for regenerating acetylcholinesterase?
Definition
Pralidoxime.
Term
What is atropine a front-line agent for?
Definition
Reversing acetylcholinesterase inhibition.
Term
What is the front-line agent for malignant hyperthermia?
Definition
Dantrolene.
Term
What is the mechanism of action of Dantrolene?
Definition
It inhibits calcium release from the SR.
Term
What is the cause of Raynaud's syndrome?
Definition
Excessive sympathetic tone in nerves supplying the hands and feet.
Term
What is the treatment for Raynaud's Syndrome?
Definition
Calcium blockers.
Term
What is the main way that norepinephrine signaling is terminated?
Definition
Neuronal uptake (70-80%).
Term
What is the mechanism of action of cocaine and tricyclic antidepressants?
Definition
They inhibit the reuptake of norepinephrine.
Term
What enzyme metabolizes re-uptooken norepinephrine in the neuron?
Definition
MAO.
Term
What enzyme metabolizes norepinephrine after extra-neuronal uptake?
Definition
COMT.
Term
Where in the cell is MAO?
Definition
Mitochondrial outer membrane.
Term
Where in the cell is COMT?
Definition
Cytosol.
Term
What MAO isoform is in the sympathetic nerves and placenta?
Definition
A.
Term
What MAO isoform is in the platelets?
Definition
B.
Term
What MAO isoform is in the liver, kidney, and brain?
Definition
A and B.
Term
List 2 effects of MAO inhibition.
Definition
Increased norepinephrine level in sympathetic neuron. Potentiated release by tyramine-like drugs.
Term
What is Tolcapone?
Definition
COMT inhibitor.
Term
What is tranylcypromine, and what is it used for?
Definition
Tranylcypromine is a non-selective MAO inhibitor used for depression.
Term
What is Selegiline, and what is it used for?
Definition
Selegiline is a MAO-B inhibitor used for Parkinson's Disease.
Term
What are VMA and MOPEG?
Definition
Major metabolites of catecholamine metabolism.
Term
List the relative affinities of epinephrine, norepinephrine, and isoproterenol for the alpha-1 receptor.
Definition
EPI > or = NE >> ISO.
Term
List the relative affinities of epinephrine, norepinephrine, and isoproterenol for the alpha-2 receptor.
Definition
NE > EPI >> ISO.
Term
List the relative affinities of epinephrine, norepinephrine, and isoproterenol for the beta-1 receptor.
Definition
ISO>EPI=NE
Term
List the relative affinities of epinephrine, norepinephrine, and isoproterenol for the beta-2 receptor.
Definition
ISO > or = EPI>>>NE.
Term
List the relative affinities of epinephrine, norepinephrine, and isoproterenol for the beta-3 receptor.
Definition
ISO=NE>EPI
Term
Does norepinephrine cross the blood brain barrier?
Definition
No.
Term
Does epinephrine cross the blood brain barrier?
Definition
No.
Term
What receptor does dopamine activate at low doses?
Definition
D.
Term
What receptor does dopamine activate at moderate doses?
Definition
Beta-1.
Term
What receptor does dopamine activate at high doses?
Definition
Alpha-1 receptors.
Term
What is Salmeterol?
Definition
Salmeterol is a LABA. It is a long-acting beta-2 agonist used for treatment of asthma and COPD.
Term
What is Terbutaline, and what is it used for?
Definition
Terbutaline is a beta-2 selective agonist used for asthma and premature labor.
Term
What is dexmedetomidine, and what is it used for?
Definition
It is an alpha-2 agonist that has CNS action and is used for sedation/analgesia in surgery.
Term
What is a cause for caution in Dexmedetomidine use?
Definition
Hypovolemic patient.
Term
What is Tizanidine, and what is it used for?
Definition
Tizanidine is an alpha-2 agonist used to treat muscle spasticity and multiple sclerosis.
Term
What is a contraindication for Tizanidine use?
Definition
CYP1A2 inhibitors.
Term
What is Pramiprexole?
Definition
A dopamine agonist used to treat Parkinson's Disease and restless leg syndrome.
Term
What is the first treatment that is typically used for Parkinson's Disease?
Definition
L-dopa/carbidopa.
Term
What is the purpose of carbidopa?
Definition
It is a decarboxylase inhibitor that cannot cross the blood brain barrier. It prevents L-dopa from being converted into dopamine until it reaches the CNS.
Term
What is Benztropine, and what is it used for?
Definition
It is a cholinoceptor antagonist that is used for Parkinson's disease.
Term
What are amphetamines used for, and what is their mechanism of action?
Definition
Amphetamines are used for narcolepsy, ADHD, and appetite suppression. They work by displacing norepinephrine.
Term
What class of drugs is methylpenidate in?
Definition
Methylpenidate is an amphetamine.
Term
What is the use of Ephedrine, and what is its mechanism of action?
Definition
Ephedrine is used as a nasal decongestant. It has direct action on alpha and beta receptors and indirect action to release norepinephrine.
Term
What types of drugs does Ephedrine interact with?
Definition
MAOI and TCA.
Term
What is the mechanism of action of tyramine?
Definition
It displaces neurotransmitter.
Term
What does tyramine interact with?
Definition
MAOI.
Term
What is a side effect of using MAOI and consuming foods high in tyramine?
Definition
Hypertension.
Term
Briefly define tachyphylaxis.
Definition
Tachyphylaxis is a short-term decrease in response to a drug due to local depletion of neurotransmitter.
Term
What class of drugs is susceptible to tachyphylaxis?
Definition
Amphetamines.
Term
List the four effects involved in the mechanism of action of amphetamine and amphetamine-like stimulants.
Definition
1. Binding to extracellular catecholamine receptors.
2. Inhibition of monoamine neurotransmitter uptake.
3. Release of catecholamines from neurons.
4. Inhibition of monoamine oxidase.
Term
What is the mechanism of action of cocaine?
Definition
It inhibits neuronal uptake.
Term
What is the mechanism of action of tricyclic antidepressants?
Definition
They inhibit neuronal uptake.
Term
What is Imipramine, and how does it work?
Definition
Imipramine is a tricyclic antidepressant that works by blocking neuronal uptake of norepinephrine.
Term
What is Amitriptylline, and how does it work?
Definition
Amitriptylline is a tricyclic antidepressant that works by blocking neuronal uptake.
Term
List three side effects of tricyclic antidepressants.
Definition
Dry mouth, blurred vision, decreased urination.
Term
What are 3 toxic effects of high doses of tricyclic antidepressants?
Definition
Severe anticholinergic effect, respiratory depression, and PHT (alpha-block)
Term
What is Atomoxetine, and what is it used for?
Definition
Atomoxetine is a tricyclic antidepressant used for ADHD.
Term
What receptors do tricyclic antidepressants block at high doses?
Definition
Alpha, M, and histamine.
Term
What is a clinical use of COMT inhibitors?
Definition
Parkinson's disease.
Term
How do MAO inhibitors potentiate the effects of tyramine?
Definition
They block metabolism of tyramine by MAO in the liver.
Term
What is the result of tyramine interactions with MAO inhibitors?
Definition
Hypertensive crisis (increased blood pressure and heart rate).
Term
What is the treatment for a tyramine crisis?
Definition
Alpha-blockers or Labetalol (alpha, beta blocker).
Term
State an appropriate drug to use for acute congestive heart failure.
Definition
Dobutamine.
Term
State two sympathomimetics appropriate to use for cardiac heart block and cardiac arrest.
Definition
Epinephrine and isoproterenol.
Term
State an ophthalmic use of phenylephrine.
Definition
Dilate pupil.
Term
State an ophthalmic use of epinephrine.
Definition
Glaucoma treatment.
Term
What is the effect of bella-donna agents on pupil size?
Definition
Dilation.
Term
Define antagonist.
Definition
An antagonist is a drug that has high affinity but no (or low) intrinsic activity.
Term
Is phenoxybenzamine a reversible or irreversible alpha-1 antagonist?
Definition
Irreversible.
Term
Is phentolamine a reversible or irreversible alpha-1 antagonist?
Definition
Reversible.
Term
List two drugs used to treat a hypertensive crisis caused by pheochromocytoma.
Definition
Phenoxybenzamine and phentolamine.
Term
What is the treatment for benign prostate hypertrophy?
Definition
Prazosin.
Term
What is the mechanism of action of prazosin?
Definition
Alpha-1 receptor blocker.
Term
What are two side-effects of phenoxybenzamine?
Definition
Orthostatic hypotension and reflex tachycardia.
Term
Describe the selectivity of phentolamine.
Definition
Equally selective for alpha-1 and alpha-2 receptors.
Term
What is the effect of beta blockers on total peripheral resistance and cardiac output?
Definition
Gradual decrease in TPR despite long-term decrease in CO.
Term
List four ways that beta-blockers are effective for hypertension treatment.
Definition
CNS action to reduce sympathetic tone.
Block of cardiac beta receptors.
Block of presynaptic beta receptors to decrease NE release.
Decrease in renin release.
Term
What type of drug is commonly used for angina?
Definition
Beta-blockers.
Term
What type of drug is often used for arrhythmia?
Definition
Beta-1 selective antagonists.
Term
What type of drug can be used to treat tremor of peripheral origin?
Definition
Beta-blocker.
Term
What type of drug can be used for migraine prophylaxis?
Definition
Beta-blocker.
Term
What drug is used in hyperthyroidism to decrease cardiac manifestation?
Definition
Propranolol.
Term
What type of drug is used to treat panic attacks and stage fright?
Definition
Beta-blocker.
Term
Which beta-blocker is not used to treat hypertension?
Definition
Esmolol (it is too short-acting).
Term
List two uses of carvedilol.
Definition
Hypertension and heart failure.
Term
What is unique about the specificity of carvedilol and labetalol?
Definition
They have alpha and beta-blocking activity.
Term
List two uses of labetalol.
Definition
Hypertension and angina.
Term
List two uses of pindolol.
Definition
Hypertension and angina.
Term
List four uses of propranolol.
Definition
Hypertension, angina, arrhythmia, and myocardial infarction (never for heart failure).
Term
In addition to glaucoma, what are four other conditions that timolol can treat?
Definition
Hypertension, angina, arrhythmia, and myocardial infarction.
Term
What are four uses of atenolol?
Definition
Hypertension, angina, arrhythmia, and myocardial infarction.
Term
What is a contraindication for using atenolol?
Definition
Pregnancy.
Term
What is esmolol used for?
Definition
Operative arrhythmia (short-acting).
Term
What are five uses of metoprolol?
Definition
Hypertension, angina, arrhythmia, myocardial infarction, and heart failure.
Term
What is nebivolol used for?
Definition
It acts as a vasodilator (via NO) and is used for hypertension.
Term
What is nebivolol selective for if less than 10 mg is used?
Definition
Beta-1 receptors.
Term
Which beta-blockers have less risk of rebound hypertension?
Definition
Beta-blockers with partial agonist activity.
Term
What type of beta-blocker should be used in patients with asthma?
Definition
Only beta-1 selective.
Term
What type of beta-blocker is preferred for patients with diabetes?
Definition
Beta-1 selective, due to blocking of beta-2 receptors in the liver.
Term
What is the effect of beta-blockers on Raynaud's disease?
Definition
May induce or worsen.
Term
What are three CNS side-effects of beta-blockers?
Definition
Nightmares, depression, and insomnia.
Term
How do the effectiveness and risk for adverse effects from beta-blockers in elderly patients compare with the effectiveness and risk of adverse effects in young patients?
Definition
Beta-blockers are less effective and more risky for older patients.
Term
What is haloperidol, and what is it used for?
Definition
Haloperidol is a dopamine antagonist used for schizophrenia and nausea.
Term
What are two side-effects of haloperidol?
Definition
Tachycardia and hypo/hypertension.
Term
What is the mechanism of action of hemicholinium?
Definition
It inhibits choline uptake into the presynaptic neuron.
Term
What is the mechanism of action of botulinum?
Definition
It inhibits acetylcholine release.
Term
What is the rate-limiting step of cholinergic neurotransmission?
Definition
Uptake of choline into the nerve terminal.
Term
What enzyme synthesizes acetylcholine?
Definition
Choline acetyltransferase.
Term
How is cholinergic neurotransmission terminated?
Definition
Acetylcholinesterase.
Term
What type of acetylcholinesterase is at the nerves and neuromuscular junction?
Definition
True acetylcholinesterase.
Term
What type of acetylcholinesterase is in the circulation?
Definition
Circulating (not true).
Term
What receptors does acetylcholine act on?
Definition
Muscarinic and nicotinic.
Term
State two uses of bethanechol.
Definition
Atonic gut and urinary retention.
Term
What receptors does bethanechol act on?
Definition
M.
Term
What is methacholine used for?
Definition
Ocular procedures.
Term
What class of drugs does methacholine belong to?
Definition
Cholinoceptor agonists (M agonist).
Term
What class of drugs does carbachol belong to?
Definition
Cholinoceptor agonist (M/some N).
Term
What is carbachol used for?
Definition
Glaucoma if pilocarpine is ineffective.
Term
What is the mechanism of action of muscarine?
Definition
Muscarinic receptor agonist.
Term
What is the drug of choice for emergency glaucoma?
Definition
Pilocarpine.
Term
What class of drugs does pilocarpine belong to?
Definition
M agonist.
Term
What muscarinic receptor agonist is diagnostic for belladonna poisoning?
Definition
Methacholine.
Term
List eight symptoms of muscarinic excess.
Definition
Diarrhea
Urination
Miosis
Bronchorrea (increased mucus)
Bradycardia
Emesis
Lacrimation
Salivation/sweating
Term
List five symptoms of nicotinic excess.
Definition
Mydriasis
Tachycardia
Weakness
Hyperthermia
Fasciculations
Term
What class of drugs does nicotine belong to?
Definition
Nicotinic receptor agonist.
Term
What is varenicline used for?
Definition
Smoking cessation.
Term
What is the mechanism of action of varenicline?
Definition
N-partial agonist.
Term
Is physostigmine a reversible or irreversible acetylcholinesterase inhibitor?
Definition
Reversible.
Term
Are organophosphates reversible or irreversible acetylcholinesterase inhibitors?
Definition
Irreversible.
Term
What drug is used to test for myasthenia gravis?
Definition
Edrophonium.
Term
What class of drugs does edrophonium belong to?
Definition
Reversible acetylcholinesterase inhibitors (quaternary ammonium compounds).
Term
What class of drugs do physostigmine and neostigmine belong to?
Definition
Reversible acetylcholinesterase inhibitors (carbamates).
Term
Of physostigmine and neostigmine, which has CNS activity?
Definition
Physostigmine.
Term
What drug is used to reverse atropine toxicity?
Definition
Physostigmine.
Term
What are two uses of neostigmine?
Definition
Reverse NMJ block and treat myasthenia gravis.
Term
What is donepezil used for?
Definition
Treatment of the symptoms of Alzheimer's disease.
Term
What is the mechanism of action of donepezil?
Definition
It is a reversible acetylcholinesterase inhibitor that has CNS activity.
Term
What is DFP used for?
Definition
Glaucoma.
Term
What is the mechanism of action of DFP?
Definition
It is an irreversible acetylcholinesterase inhibitor.
Term
What is echothiophate used for?
Definition
Glaucoma.
Term
What is the mechanism of action of echothiophate?
Definition
Irreversible acetylcholinesterase inhibitor.
Term
Does echothiophate have CNS activity?
Definition
No.
Term
What is the mechanism of action of nerve gases?
Definition
Irreversible acetylcholinesterase inhibitors.
Term
What are malathion and parathion?
Definition
Irreversible acetylcholinesterase inhibitors used in insecticides.
Term
What is the purpose of 2-PAM?
Definition
It can reverse the inhibition of acetylcholinesterase by organophosphates before aging has occurred.
Term
Rank DFP, nerve gas, and insecticides from shortest to longest aging process.
Definition
Nerve gas, DFP, insecticides.
Term
What type of glaucoma can be treated with physostigmine and echothiophate?
Definition
Wide-angle or secondary.
Term
What is the preferred drug to use for treatment of toxicity due to high concentrations of tricyclic antidepressants?
Definition
Physostigmine.
Term
What is the mechanism of action of atropine?
Definition
It blocks acetylcholine in parasympathetic effector junctions (muscarinic receptors).
Term
What is the mechanism of action of trimethapan?
Definition
It blocks acetylcholine in ganglia(both parasympathetic and sympathetic).
Term
What is the mechanism of action of curare and succinylcholine?
Definition
They block acetylcholine at the neuromuscular junction (skeletal muscle relaxants).
Term
What is the effect of anticholinergic agents on the heart?
Definition
Tachycardia and increased A-V nodal CV.
Term
What is the effect of anticholinergic agents on the vasculature?
Definition
No effect (vasodilation at toxic doses, though).
Term
What is the effect of anticholinergic agents on the GI tract and urinary tract?
Definition
Relaxation, decreased secretion, decreased motility.
Term
What is the effect of anticholinergic agents on the lungs?
Definition
Bronchial relaxation and decreased bronchial secretions.
Term
What is the effect of anticholinergic agents on the eye?
Definition
Mydriasis (sphincter relaxation)
Cyclopegia (ciliary muscle relaxation)
Term
What is the effect of anticholinergic agents on the CNS?
Definition
Agitation, delirium, confusion.
Term
What is scopolamine used for?
Definition
Motion sickness.
Term
What is the mechanism of action of scopolamine?
Definition
Antimuscarinic agent (like atropine).
Term
What is ipratropium used for?
Definition
Asthma and COPD.
Term
What is the mechanism of action of ipratropium?
Definition
Antimuscarinic.
Term
What is tiotropium used for?
Definition
Asthma and COPD.
Term
What is the mechanism of action of tiotropium?
Definition
Antimuscarinic.
Term
What is benztropine used for?
Definition
Parkinson's disease.
Term
What is the mechanism of action of benztropine?
Definition
Antimuscarinic.
Term
What is propantheline used for?
Definition
GI disorders.
Term
What is the mechanism of action of propantheline?
Definition
Antimuscarinic.
Term
List four clinical uses of botulinus toxin.
Definition
Facial muscle spasms, strabismus, wrinkles, and migraine.
Term
What is the treatment for atropine toxicity?
Definition
Neostigmine or physostigmine.
For hypotension, sympathomimetics (alpha agonist like methoxamine).
Term
List six symptoms of antimuscarinic toxicity.
Definition
Mad as a hatter: CNS, delirium.
Red as a beet: Direct vasodilation.
Blind as a bat: Cycloplegia.
Hot as a hare: Decreased sweat, thermoregulation.
Dry as a bone: Decreased secretion.
At high concentrations, hypotension due to ganglionic block.
Term
How do carbonic acid inhibitors treat glaucoma?
Definition
Decrease secretion.
Term
What is latanoprost used for?
Definition
Glaucoma.
Term
How does latanoprost work?
Definition
It is a prostaglandin analogue that treats glaucoma by increasing outflow. It also produces fuller lashes.
Term
What is dorzolamide used for?
Definition
Glaucoma.
Term
What is the mechanism of action of dorzolamide?
Definition
It is a prostaglandin analogue that treats glaucoma by decreasing aqueous formation.
Term
What glaucoma drug is contraindicated for patients with a sulfa drug allergy?
Definition
Dorzolamide.
Term
What is pyridostigmine used for?
Definition
Myasthenia gravis.
Term
What is the mechanism of action of pyridostigmine?
Definition
Reversible acetylcholinesterase inhibition.
Term
What is mecamylamine?
Definition
It is an oral ganglionic blocking agent used to decrease blood pressure during surgery.
Term
Define absorption.
Definition
The process of movement of a drug from its site of administration into plasma.
Term
Define distribution.
Definition
Movement of a drug from plasma into tissues and back.
Term
What is the formula for the rate of diffusion of a drug across a lipid membrane?
Definition
Rate of diffusion = -DAK(delta C)/Thickness.
Term
What is the relationship between rate of filtration and drug concentration?
Definition
Rate is directly proportional to drug concentration (1st order).
Term
What is the equation for the half-life for drug absorption?
Definition
T1/2,ab = 0.693/Kab
Term
What is the formula for the amount of drug absorbed?
Definition
Amount absorbed = F x D.
Term
How can adverse systemic effects of local anesthetics be minimized?
Definition
Use vasoconstrictors to reduce blood flow to the site of administration and reduce absorption into the plasma.
Term
What is the main site of absorption for oral drugs?
Definition
Small intestine.
Term
What is the formula for bioavailability of a drug taken orally?
Definition
F = AUC oral/AUC injected x 100
Term
What does metoclopramide do?
Definition
It enhances gastric emptying rate.
Term
What is the pharmacokinetic effect of antacids?
Definition
Antacids affect the absorption of drugs requiring gastric fluid acidity for dissolution and form unabsorbable complexes with drugs in the gastrointestinal tract.
Term
What is the pharmacokinetic effect of proton pump inhibitors?
Definition
Proton pump inhibitors affect the absorption of drugs requiring gastric fluid acidity for dissolution.
Term
What is the pharmacokinetic effect of cholestyramine?
Definition
Cholestyramine affects absorption by adsorbing drugs in the gastrointestinal tract.
Term
What is the pharmacokinetic effect of iron?
Definition
Iron forms unabsorbable complexes with drugs in the gastrointestinal tract.
Term
Where are fenestrated capillary beds located?
Definition
Most tissues, including the kidney.
Term
What types of drugs can pass through fenestrated capillary beds?
Definition
Unbound drugs that do not have a large molecular weight.
Term
Where are sinusoidal capillary beds located?
Definition
In the liver.
Term
List three locations of closed capillary beds.
Definition
Brain, placenta, testes.
Term
How can drugs pass through continuous (closed) capillary beds?
Definition
Only by lipid diffusion or carrier-mediated transport.
Term
What is thiopental used for?
Definition
It is used as a sedative/hypnotic.
Term
Why is thiopental an effective inducer of anesthesia?
Definition
It distributes rapidly to the brain because it is a highly perfused tissue.
Term
Why do the effects of thiopental terminate in 15-20 minutes?
Definition
Slower but more effective distribution of the drug to non-target tissues with slower perfusion (fat and lean tissues).
Term
How does the stomach function as a drug reservoir?
Definition
The low pH traps basic drugs.
Term
How does the liver function as a drug reservoir?
Definition
The liver avidly binds drugs (chloroquine)
Term
How do the bones and teeth act as drug reservoirs?
Definition
They bind tetracyclines and fluoroquinolones (antibacterial drugs).
Term
How does fat function as a drug reservoir?
Definition
Fat concentrates lipid soluble drugs like thiopental.
Term
What is the formula for volume of distribution?
Definition
Vd = amount of drug in the body/C
Term
What is the loading dose equation?
Definition
D = Vd x C/F
Term
What is the equation for first-order rate of elimination?
Definition
Rate of elimination = CL x C
Term
What is the equation for the rate of zero-order elimination?
Definition
Rate of elimination = k.
Term
What is the equation for clearance?
Definition
CL = rate of elimination/C
Term
What is the equation for Kel in terms of Vd and CL?
Definition
Kel = CL/Vd
Term
What ise equation for half-life in terms of CL and Vd.
Definition
T1/2 = 0.693Vd/CL
Term
What type of elimination kinetics is followed by ethanol and phenytoin?
Definition
Zero-order.
Term
What are the three mechanisms that determine CLr?
Definition
Glomerular filtration.
Tubular secretion.
Tubular reabsorption.
Term
What is the equation for CL GF?
Definition
CL GF = (Fraction of drug unbound in plasma)(GFR)
Term
What is the glomerular filtration rate in a healthy adult?
Definition
7.8 L/hr/70 kg
Term
What process is used to transport weak acids and weak bases on the blood-facing side in the kidney?
Definition
Facilitated diffusion.
Term
What process is used to transport drugs into the lumen of the nephron during secretion?
Definition
Active transport by multidrug resistance proteins.
Term
What is the maximum value of CL TS?
Definition
39 L/hr.
Term
What must be true if CLr > CL GF?
Definition
Secretion plays a role in elimination.
Term
What is used to estimate RPF?
Definition
Para-aminohippuric acid clearance.
Term
What is the primary method of elimination for penicillin?
Definition
Tubular secretion by OATs.
Term
What is the effect of probenecid on tubular secretion?
Definition
Probenecid is a weak acid that competes with weak acid drugs (like penicillin) for OATs.
Term
What is the effect of cimetidine on tubular secretion?
Definition
Cimetidine is a weak base that competes with other weak base drugs for OBTs.
Term
State a clinical use of sodium bicarbonate.
Definition
Sodium bicarbonate is used to alkalinize urine and increase excretion of weak acid drugs by decreasing reabsorption.
Term
State a clinical use of ammonium chloride.
Definition
Ammounium chloride is used to acidify the urine and increase the excretion of weak base drugs by decreasing reabsorption.
Term
What are the cardiovascular effects of a high dose of phenylephrine?
Definition
Increased blood pressure due to activation of alpha-1 receptors and vasoconstriction. Decreased heart rate due to reflex.
Term
What are the cardiovascular effects of epinephrine?
Definition
Increased blood pressure due to activation of alpha-1 receptors and beta-1 receptors. Increased heart rate due to activation of beta-1 receptors (attenuated by reflex bradycardia).
Term
What are the cardiovascular effects of a high dose of isoproterenol?
Definition
Decreased blood pressure due to activation of beta-2 receptors. Increased heart rate due to activation of beta-1 receptors + reflex.
Term
What are the cardiovascular effects of epinephrine after phentolamine?
Definition
Increased PP, decreased BP, increased HR (reflex).
Term
Draw the diagram of the cardiovascular effects of a high dose of norepinephrine.
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of a high dose of phenylephrine.
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of a high dose of epinephrine.
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of a high dose of isoproterenol.
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of a high dose of phentolamine (an alpha-blocker).
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of a high dose of propranolol (a beta-blocker).
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of norepinephrine + atropine.
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of norepinephrine + an alpha-blocker.
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of norepinephrine + a beta-blocker.
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of phenylephrine + atropine.
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of epinephrine + an alpha-blocker.
Definition
See notes.
Term
Draw a diagram showing the cardiovascular effects of epinephrine + a beta-blocker.
Definition
See notes.
Term
What do Phase 1 enzymes do?
Definition
Add or unmask functional group on a drug.
Term
What do Phase 2 enzymes do?
Definition
Phase 2 enzymes are conjugation enzymes that add an endogenous substance to the functional group to change the excretability or activity of a drug.
Term
Where are cytochrome P450s and glucuronosyltransferases located in the cell?
Definition
Smooth endoplasmic reticulum.
Term
What is the pharmacokinetic effect of phenobarbital?
Definition
Phenobarbital induces CYPs 2C9, 2C19, and 3A4.
Term
What is the pharmacokinetic effect of rifampin?
Definition
Inducer of CYPs 2C9, 2C19, 3A4
Term
What is the pharmacokinetic effect of phenytoin?
Definition
Inducer of CYPs 2C9, 2C19, 3A4
, example of saturable kinetics of elimination
Term
What is the pharmacokinetic effect of carbamazepine?
Definition
Inducer of CYPs 2C9, 2C19,
3A4
Term
What is the pharmacokinetic effect of cigarette smoke?
Definition
Inducer of CYP1A2.
Term
What is the pharmacokinetic effect of alcohol?
Definition
Inducer of CYP2E1.
Term
What is the pharmacokinetic effect of St. John's wort?
Definition
Inducer of CYPs 2C9, 2C19, 3A4
Term
What is the effect of cimetidine on drug metabolism?
Definition
Broad spectrum inhibitor of many cytochrome P450s.
Term
What is the pharmacokinetic effect of azole antifungals?
Definition
Inhibitors of CYP2C9 and CYP3A4
Term
What is the pharmacokinetic effect of macrolide antibacterials?
Definition
Inhibitors of CYP3A4.
Term
What is the pharmacokinetic effect of HIV protease inhibitors?
Definition
Inhibitors of CYP3A4.
Term
What is the pharmacokinetic effect of grapefruit juice?
Definition
Inhibitor of CYP3A4 (intestinal form only).
Term
What cytochrome metabolizes theophylline?
Definition
CYP1A2.
Term
What cytochrome metabolizes warfarin?
Definition
CYP2C9.
Term
What are the effects of cholestasis and choleresis on CLbiliary?
Definition
Cholestasis decreases CLbiliary. Choleresis increases CLbiliary.
Term
What is the approximate CLh of high hepatic extraction drugs?
Definition
90 L/hr.
Term
Do inducers and inhibitors of drug metabolism have a high effect on high hepatic extraction drugs?
Definition
No.
Term
Is the CLh of low hepatic extraction drugs highly affected by inducers or inhibitors of drug metabolism?
Definition
Yes.
Term
What is the mechanism of carbon monoxide toxicity?
Definition
It binds to iron in hemoglobin, myoglobin, and cytochrome oxidase. It binds to hemoglobin with a higher affinity than oxygen.
Term
What is the effect of carbon monoxide on the hemoglobin saturation curve?
Definition
Shift to the left.
Term
What is the effect of CO toxicity on blood pressure?
Definition
Hypotension due to myocardial toxicity and peripheral vasodilation.
Term
What is the effect of CO toxicity on blood pH?
Definition
Metabolic acidosis.
Term
What are the symptoms of amphetamine toxicity?
Definition
Sympathomimetic toxidrome.
Term
What class of drugs is used to treat amphetamine toxicity?
Definition
Benzodiazepines.
Term
What toxicity is treated with midazolam, lorazepam and diazepam?
Definition
Amphetamine toxicity.
Term
Which CYP enzyme system makes the toxic metabolite from acetaminophen?
Definition
CYP2E1.
Term
What stage of acetaminophen toxicity is characterized by nausea, vomiting, epigastric pain, pallor, and diaphoresis?
Definition
Stage 1 (30 minutes to 24 hours).
Term
In what stage of acetaminophen toxicity do lab abnormalities and RUQ pain begin?
Definition
Stage 2.
Term
In what stage of acetaminophen toxicity do liver and kidney failure develop and lab abnormalities peak?
Definition
Stage 3 (72 to 96 hours).
Term
What stage of acetaminophen toxicity involves either death or resolution?
Definition
Stage 4.
Term
At 4 hours after acetaminophen ingestion, what acetaminophen level warrants treatment?
Definition
150 micrograms per milliliter.
Term
What is the treatment for acetaminophen toxicity?
Definition
N-acetylcysteine.
Term
What is the mechanism of action of NAC?
Definition
NAC is converted to glutathione and converts NAPQI into nontoxic metabolites.
Term
What is the mechanism of toxicity of aspirin?
Definition
It uncouples oxidative phosphorylation.
Term
What toxicity causes high anion gap metabolic acidosis and respiratory alkalosis?
Definition
Aspirin.
Term
What toxicity causes tinnitus, hearing loss, hallucinations, agitation, coma, and seizures?
Definition
Aspirin.
Term
What is the treatment of aspirin toxicity?
Definition
Sodium bicarbonate infusion.
Term
What is the renal toxic metabolite of ethylene glycol?
Definition
Oxalic acid.
Term
How soon do you see evidence of renal failure after ethylene glycol poisoning?
Definition
24 hours.
Term
What antidote was previously used to treat ethylene glycol poisoning?
Definition
Ethanol (alcohol dehydrogenase inhibitor).
Term
What is the treatment for ethylene glycol toxicity?
Definition
Fomepizole.
Term
What is the mechanism of toxicity of lead?
Definition
It binds to proteins and enzymes.
Term
What toxicity is associated with a decrease in IQ?
Definition
Lead.
Term
What toxicity is associated with basophilic stippling?
Definition
Lead.
Term
What toxicity is associated with hypertension, chromosomal abnormalities, decreased testicular function, delayed menses, colicky pain, and constipation?
Definition
Lead.
Term
What is the most effective method to treat chronic lead exposure?
Definition
Removal from exposure.
Term
What is the toxic metabolite of methanol?
Definition
Formaldehyde and formic acid.
Term
What toxicity is associated with visual symptoms, such as snow storm vision, within 24 hours?
Definition
Methanol.
Term
What is the mechanism of toxicity of cyanide?
Definition
It binds to cytochrome oxidase and inhibits ATP production. It also decreases the use of oxygen, resulting in bright red venous blood.
Term
What is the treatment for methanol poisoning?
Definition
Fomepizole.
Term
What is the pharmacological treatment for lead poisoning?
Definition
Succimer.
Term
What is the major symptom of CO poisoning?
Definition
Headache.
Term
What is the treatment for CO poisoning?
Definition
Oxygen.
Term
What is the major symptom of CN poisoning?
Definition
Syncope.
Term
What is the treatment for CN poisoning?
Definition
Hydroxycobalamin.
Term
Does tubocurarine cause histamine release?
Definition
Yes.
Term
Does tubocurarine block ganglionic receptors?
Definition
Yes, at high concentrations.
Term
How does the histamine release of pancuronium compare with the histamine release by tubocurarine?
Definition
Less histamine is released by pancuronium.
Term
Does pancuronium cause a ganglionic blockade?
Definition
No.
Term
What is important about the onset of rocuronium?
Definition
Rocuronium has fast onset (1-2 minutes).
Term
What is the advantage of cisatracurium?
Definition
It is degraded by organ-independent Hoffmann degradation.
Term
How is toxicity of competitive neuromuscular junction antagonists reversed?
Definition
Acetylcholinesterase inhibitors such as neostigmine.
Term
Does succinylcholine cause more or less histamine release and ganglionic blocking than tubocurarine?
Definition
Less.
Term
Are the effects of succinylcholine reversed by acetylcholinesterase inhibitors?
Definition
No.
Term
What is the treatment for succinylcholine toxicity?
Definition
Artificial respiration.
Term
List three adverse effects of succinylcholine.
Definition
Apnea in patients with atypical pseudo-acetylcholinesterase.
Hyperkalemia, especially in burn and trauma patients, 2-7 hours after use.
Malignant hyperthermia.
Term
What drug increases the likelihood of malignant hyperthermia caused by succinylcholine?
Definition
Halothane.
Term
What drug is used to treat malignant hyperthermia?
Definition
Dantrolene.
Term
What is the mechanism of action of dantrolene?
Definition
Decrease calcium release.
Term
How do calcium channel blockers like verapamil interact with NMJ blocking agents?
Definition
Decrease acetylcholine release.
Term
How do aminoglycoside antibiotics interact with NMJ blockers?
Definition
They compete with calcium to decrease acetylcholine release and stabilize the membrane.
Term
How do certain general anesthetics such as halothane interact with NMJ blockers?
Definition
Stabilize membrane.
Term
What is the steady state rate equation?
Definition
FD/T = CL * Css.
Term
What can you conclude if EC50
Definition
Spare receptors exist.
Term
Define premature infant.
Definition
Less than 36 weeks gestation.
Term
Define full-term infant.
Definition
36-40 weeks gestation.
Term
Define neonate.
Definition
First 4 weeks postnatal.
Term
Define infant.
Definition
5-32 weeks postnatal.
Term
Define children.
Definition
1-12 years.
Term
Define adolescents.
Definition
12-16 years.
Term
What is the formula for therapeutic index?
Definition
TI = LD50/ED50.
Term
What is the equation for Certain Safety Factor?
Definition
CSF = LD1/ED99.
Term
Define geriatrics.
Definition
Older than 65.
Term
Compare the elimination half-life of diazepam in neonates, infants, and adults.
Definition
The elimination half-life of diazepam is greatest in neonates and the elderly and shortest in infants/children.
Term
List the steps of drug development and testing.
Definition
In vitro studies, animal testing, phase 1-3 clinical trials, postmarketing surveillance.
Term
What is the goal of phase 1 clinical trials?
Definition
Establish limits of safe clinical dosage range.
Term
What is done in phase 2 clinical trials?
Definition
The drug is tested in a small number of patients with the target disease to determine the efficacy, safety, and optimum dose.
Term
What is done in phase 3 clinical trials?
Definition
The drug is studied in a large number of patients to further establish the safety and efficacy.
Term
When is a New Drug Application filed?
Definition
After the clinical trials.
Term
Explain the important polymorphism of the beta-2 adrenergic receptor discussed in class.
Definition
Individuals with the G16 variant (60% of Hispanic/Caucasian individuals) down-regulate the beta-2 adrenergic receptor in response to agonists. Albuterol is less effective in G16 individuals.
Term
As discussed in class, a polymorphism in what cytochrome P450 enzyme leads to unusual responses to phenytoin?
Definition
CYP2C19.
Term
As discussed in class, a polymorphism in what cytochrome P450 enzyme affects the appropriate dose of warfarin?
Definition
CYP2C9.
Term
What cytochrome P450 enzyme metabolizes codeine into morphine?
Definition
CYP2D6.
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