Pharm 1 FInal Review
A. It will go up
The drug from the previous question is given to a patient with severe liver failure. What, if any, change in the volume of distribution will there be in this patient. A. It will go up B. It will stay the same C. It will go down
Methacholime
Used to DIAGNOSE asthma
tripicamide
What dilates the eye for 2 hours
Atropine
What drug is a last resort because of its long acting effects on the eyes? And CI with closed angle glaucoma
Increased risk of toxicity
What is a disadvantage of giving a pt a loading dose?
Succinylcholine
What medication can cause malignant hyperthermia to which dantrolene is the antidote
A. Tropium
What muscarinic antagonist is best for treating overactive bladder and urinary incontinence in dementia patients? A. Tropium B. Oxybutynin C. Fesoterodine D. Darifenacin
4-5 half lives
When determining maintenance dose how many half lives does it take to obtain the steady state (w/o loading dose)
Correct answer = A. Vd = dose/C = 2000 mg/28.5 mg/L = 70.1 L. Because the patient is 70 kg, the apparent vol- ume of distribution in L/kg will be approximately 1 L/kg (70.1 L/70 kg).
A 40-year-old male patient (70 kg) was recently diagnosed with infection involving methicillin-resistant S. aureus. He received 2000 mg of vancomycin as an IV loading dose. The peak plasma concentration of vancomycin was reported to be 28.5 mg/L. The apparent volume of distribution is: A. 1 L/kg. B. 10 L/kg. C. 7 L/kg. D. 70 L/kg. E. 14 L/kg.
Correct answer = A. For IV infusion, Loading dose = (Vd) × (desired steady-state plasma concentration). The Vd in this case corrected to the patient's weight is 70 L. Thus, Loading dose = 70 L × 2.5 mg/L = 175 mg.
A 55-year-old male patient (70 kg) is going to be treated with an experimental drug, Drug X, for an irregular heart rhythm. If the Vd is 1 L/kg and the desired steady-state plasma concentration is 2.5 mg/L, which of the following is the most appropriate intravenous loading dose for Drug X? A. 175 mg. B. 70 mg. C. 28 mg. D. 10 mg. E. 1 mg.
D. Sublingual
A 6 year-old male presents to the ED with intractable vomiting. The patient is alert and oriented and is showing signs of mild dehydration. Which of the following routes is the most appropriate to deliver ondansetron, a 5-HT3 receptor antagonist for nausea and vommitting? A) Oral B) Intravenous C) Intramuscular D) Sublingual E) Intrathecal
E. 400 mg (60kg • 2L/kg = 120L —> LD = 120 • [3/0.9]) —> 400
A 64 year-old female (60 kg) is treated with Drug A for infection. Drug A is available in tablets with an oral bioavailability of 90%. If the Vd is 2L/kg and the desired steady state concentration is 3 mg/L, which of the following is the most appropriate loading dose of drug A? A. 6 mg B. 6.66 mg C. 108 mg D. 360 mg E. 400 mg
Correct answer = E. Clopidogrel is a prodrug, and it is acti- vated by CYP2C19, which is a cytochrome P450 (CYP450) enzyme. Thus, patients who are poor CYP2C19 metabo- lizers have a higher incidence of cardiovascular events (for example, stroke or myocardial infarction) when taking clopidogrel.
A 65-year-old female patient (60 kg) with a history of ischemic stroke was prescribed clopidogrel for stroke prevention. She was hospitalized again after 6 months due to recurrent ischemic stroke. Which of the following is a likely reason she did not respond to clopidogrel therapy? She is a: A. Poor CYP2D6 metabolizer. B. Fast CYP1A2 metabolizer. C. Poor CYP2E1 metabolizer. D. Fast CYP3A4 metabolizer. E. Poor CYP2C19 metabolizer.
C. Reduced antiplatelet activity of clopidogrel due to omeprazole
A 68 year-old woman is brought to the ER for a myocardial infarction. She is taking clopidogrel (antiplatelet) and aspirin daily, as well as omeprazole (a potent CYP inhibitor) for heartburn. Which of the following is a likely contributor to her heart attack today? A. Reduced antiplatelet activity of clopidogrel due to aspirin B. Hypersensitivity reaction to clopidogrel C. Reduced antiplatelet activity of clopidogrel due to omeprazole D. Increased antiplatelet activity of clopidogrel due to omeprazole
Correct answer = D. Salivary glands contain muscarinic receptors, not nicotinic receptors. Activation of muscarinic receptors in the salivary glands causes secretion of saliva. Blocking muscarinic receptors, using drugs such as atro- pine, reduces salivary secretions and makes the mouth dry.
A dentist would like to reduce salivation in a patient in preparation for an oral surgical procedure. Which of the following strategies will be useful in reducing salivation? A. Activate nicotinic receptors in the salivary glands. B. Block nicotinic receptors in the salivary glands. C. Activate muscarinic receptors in the salivary glands. D. Block muscarinic receptors in the salivary glands
Correct answer = D. A drug will reach steady state in about four to five half-lives. Thus, for this drug with a half-life of 10 hours, the approximate time to reach steady state will be 40 hours.
A drug with a half-life of 10 hours is administered by continuous intravenous infusion. Which of the following best approximates the time for the drug to reach steady state? A. 10 hours. B. 20 hours. C. 33 hours. D. 40 hours. E. 60 hours
A. Clearance of amphetamine will be increased
A patient is taking amphetamine, a weak base. The patient begins taking ascorbic acid because they heard that acidifying the urine prevents UTIs. Which of the following is a likely outcome? A) The clearance of amphetamine will be increased B) The clearance of amphetamine will be decreased C) The clearance of amphetamine will not be affected D) The clearance of ascorbic acid will be increased
B. Administer bicarbonate to alkalinity the urine
A patient presents with phenobarbital (weak acid) overdose symptoms. Which of the following will promote clearance of the drug? A) Administer ascorbic acid to acidify the urine B) Administer bicarbonate to alkalinize the urine C) Administer ascorbic acid to alkalinize the urine D) Administer bicarbonate to acidify the urine
Doneprezil
AChE inhibitor. Treats Alzheimers.
Correct answer = B. When there is a sudden drop in blood pressure, the baroreceptors send signals to the brain, and the brain activates the sympathetic system (not the para- sympathetic system) to restore blood pressure to normal values.
All of the following statements regarding central control of autonomic functions are correct except: A. Baroreceptors are pressure sensors located at various cardiovascular sites. B. The parasympathetic system is activated by the CNS in response to a sudden drop in blood pressure. C. The parasympathetic system is activated by the CNS in response to a sudden increase in blood pressure. D. The sympathetic system is activated by the CNS in response to a sudden drop in blood pressure.
Correct answer = E. The intravenous route of administration is the most desirable because it results in achievement of therapeutic plasma levels of the antidote rapidly
An 18-year-old female patient is brought to the emergency department due to drug overdose. Which of the following routes of administration is the most desirable for administering the antidote for the drug overdose? A. Intramuscular. B. Subcutaneous. C. Transdermal. D. Oral. E. Intravenous.
Correct answer D. Basic drugs deprotonated when pH greater than the pKa (greater than 7.8)
Drug A is a weakly basic drug with a pKa of 7.8. If given orally, at which of the following sites will the drug be able to readily cross through the membrane? A) Mouth (pH around 7) B) Stomach (pH 2.5) C) Duodenum (pH 6.1) D) Jejunum (pH 8) E) Ileum (pH 7)
Correct answer = B. Activation of α1 receptors causes mydriasis, vasoconstriction, and an increase in blood pres- sure. Activation of β1 receptors increases heart rate, con- tractility of the heart, and blood pressure. Activation of β2 receptors causes dilation of bronchioles and relaxation of skeletal muscle vessels. Thus, inhibition of these receptors will cause vasorelaxation (α1 blockade), reduction in heart rate (β1 blockade), reduction in contractility of the heart (β1 blockade), reduction in blood pressure, bronchoconstric- tion (β2 blockade), and constriction of blood vessels supply- ing skeletal muscles (β2 blockade)
An elderly man was brought to the emergency room after he ingested a large quantity of carvedilol tablets, a drug that blocks α1, β1, and β2 adrenergic receptors, which mainly mediate the cardiovascular effects of epinephrine and norepinephrine in the body. Which of the following symptoms would you expect in this patient? A. Increased heart rate (tachycardia). B. Reduced heart rate (bradycardia). C. Dilation of the pupil (mydriasis). D. Increased blood pressure.
Physostigmine
Antidote for atropine toxicity
High doses
At ________ doses neuromuscular blockers cannot be reversed by AChE inhibitors nor direct electrical stimulation
bronchodilation
Beta 2 agonist response
Correct answer = B. Because chlorothiazide is a weakly acidic drug (pKa = 6.5), it will be predominantly in non- ionized form in the stomach (pH of 2.5). For weak acids, the nonionized form will permeate through cell membrane readily
Chlorothiazide is a weakly acidic drug with a pKa of 6.5. If administered orally, at which of the following sites of absorption will the drug be able to readily pass through the membrane? A. Mouth (pH approximately 7.0). B. Stomach (pH of 2.5). C. Duodenum (pH approximately 6.1). D. Jejunum (pH approximately 8.0). E. Ileum (pH approximately 7.0)
muscarinic receptors
Cholinergic receptors that are located postsynaptically in the effector organs such as smooth muscle, cardiac muscle, and glands supplied by parasympathetic fibers.
A 30-year-old male patient was brought to the ER with amphetamine overdose. He presented with high blood pressure and arrhythmia. Which of the following is correct regarding this patient? A. Amphetamine can activate all types of adrenergic receptors. B. β-Blockers are the ideal antidotes for amphetamine poisoning. C. α-Blockers can normalize the blood pressure in this patient. D. Miosis could be a possible symptom of amphetamine poisoning.
Correct answer = A. Amphetamine is an indirect adrenergic agonist that mainly enhances the release of norepinephrine from peripheral sympathetic neurons. Therefore, it activates all types of adrenergic receptors (that is, α and β receptors) and causes an increase in blood pressure. Since both α and β receptors are activated by amphetamine, α-blockers or β-blockers alone cannot relieve the symptoms of amphet- amine poisoning. Since amphetamine causes sympathetic activation, it causes mydriasis, not miosis.
Which of the following is correct regarding β-blockers? A. Treatment with β-blockers should not be stopped abruptly. B. Propranolol is a cardioselective β-blocker. C. β-Blockers may cause orthostatic hypotension. D. Cardioselective β-blockers worsen asthma. E. β-Blockers decrease peripheral resistance by causing vasorelaxation.
Correct answer = A. If β-blocker therapy is stopped abruptly, that could cause angina and rebound hypertension. This could be due to the up-regulation of β receptors in the body. β-Blockers do not cause direct vasorelaxation. Therefore, they do not decrease peripheral resistance and are less likely to cause orthostatic hypotension. Propranolol is a nonselective β-blocker (not cardioselective). Cardioselective β-blockers antagonize only β1 receptors and do not worsen asthma as they do not antagonize β2 receptors.
Which of the following is correct regarding responses mediated by adrenergic receptors? A. Stimulation of α1 receptors increases blood pressure. B. Stimulation of α receptors reduces blood pressure. C. Stimulation of sympathetic presynaptic α receptors increases norepinephrine release. D. Stimulation of β2 receptors increases heart rate (tachycardia). E. Stimulation of β2 receptors causes bronchoconstriction.
Correct answer = A. Stimulation of α1 receptors, mostly found in the blood vessels, causes vasoconstriction and increase in blood pressure. Stimulation of α2 receptors on the sympathetic presynaptic terminal reduces the release of norepinephrine. β2 receptors are not found in the heart, so activation of β receptors does not affect heart rate. Stimulation of β2 receptors found in the bronchial tissues causes bronchodilation, not bronchoconstriction.
An asthma patient was given a nonselective β agonist to relieve bronchoconstriction. Which of the following adverse effects would you expect to see in this patient? A. Bradycardia. B. Tachycardia. C. Hypotension (reduction in blood pressure). D. Worsening bronchoconstriction
Correct answer = B. A nonselective β agonist activates both β1 as well as β2 receptors. β1 activation causes an increase in heart rate (tachycardia), contractility, and subsequent increase in blood pressure. It relieves bronchoconstriction because of the β2 receptor activation.
50-year-old male was brought to the emergency room after being stung by a hornet. The patient was found to be in anaphylactic shock, and the medical team tried to reverse the bronchoconstriction and hypotension using epinephrine. However, the patient did not fully respond to the epinephrine treatment. The patient's wife mentioned that he is taking a prescription medication for his blood pressure, the name of which she does not remember. Which of the following medications is he most likely taking that could have prevented the effects of epinephrine? A. Doxazosin. B. Propranolol. C. Metoprolol. D. Acebutolol.
Correct answer = B. Epinephrine reverses hypotension by activating β1 receptors and relieves bronchoconstriction by activating β2 receptors in anaphylaxis. Since epinephrine was not effective in reversing hypotension or bronchocon- striction in this patient, it could be assumed that the patient was on a nonselective β-blocker (propranolol). Doxazosin (α1-blocker), metoprolol, or acebutolol (both β1-selective blockers) would not have completely prevented the effects of epinephrine.
A β-Blocker was prescribed for hypertension in a female asthma patient. After about a week of treatment, the asthma attacks got worse, and the patient was asked to stop taking the β-Blocker. Which of the following β-Blockers would you suggest as an alternative in this patient that is less likely to worsen her asthma? A. Propranolol B. Metoprolol C. Labetalol D. Carvedilol
Correct answer = B. The patient was most likely given a nonselective β-blocker (antagonizes both β1 and β2 recep- tors) that made her asthma worse due to β2 antagonism. An alternative is to prescribe a cardioselective (antagonizes only β1) β-blocker that does not antagonize β2 receptors in the bronchioles. Metoprolol is a cardioselective β-blocker. Propranolol, labetalol, and carvedilol are nonselective β-blockers and could worsen the asthma.
Which of the following is correct regarding α-adrenergic blockers? A. α-Adrenergic blockers are used in the treatment of hypotension in anaphylactic shock. B. α-Adrenergic blockers are used in the treatment of benign prostatic hyperplasia (BPH). C. α-Adrenergic blockers may cause bradycardia. D. α-Adrenergic blockers are used in the treatment of asthma. E. α-Adrenergic blockers reduce the frequency of urination
Correct answer = B. α-Adrenergic blockers are used in the treatment of BPH because of their relaxant effect on prostate smooth muscles. Being antihypertensive agents, they are not useful in treating hypotension in anaphylaxis. α-Adrenergic blockers generally cause reflex tachycardia (not bradycardia) due to the significant drop in blood pres- sure caused by them. α-Adrenergic blockers have no sig- nificant effects on bronchial tissues and are not useful in treating asthma. They increase (not reduce) the frequency of urination by relaxing the internal sphincter of the urinary bladder, which is controlled by α1 receptors.
A hypertensive patient was accidentally given an α 2 agonist instead of an α1 blocker. Which of the following is correct in this situation? A. α2 Agonists can increase the release of norepinephrine from sympathetic nerve terminals. B. α Agonists can reduce blood pressure in this 2 patient. C. α2 Agonists can increase blood pressure in this patient. D. α2 Agonists will not affect blood pressure in this patient.
Correct answer = B. α2 Agonists activate α2 receptors located in the presynaptic terminal of sympathetic neurons and cause a reduction in the release of norepinephrine from sympathetic nerve terminals. This leads to a reduction in blood pressure. α2 Agonists such as clonidine and methyl- dopa are therefore used as antihypertensive agents.
Which of the following drugs is commonly used topically in the treatment of glaucoma? A. Atropine. B. Timolol. C. Tropicamide. D. Scopolamine.
Correct answer = B. β-Blockers reduce the formation of aqueous humor in the eye and therefore reduce intraocular pressure, thus relieving glaucoma. Timolol is a nonselective β-blocker that is commonly used topically to treat glaucoma. Atropine, tropicamide, and scopolamine are anticholinergic drugs that might worsen glaucoma.
70-year-old patient was brought to the emergency room with a blood pressure of 76/60 mm Hg, tachycardia, and low cardiac output. He was diagnosed with acute heart failure. Which of the following drugs would be the most appropriate to improve his cardiac function? A. Epinephrine. B. Fenoldopam. C. Dobutamine. D. Isoproterenol.
Correct answer = C. Among the choices, the ideal drug to increase contractility of the heart in acute heart failure is dobutamine, since it is a selective β1-adrenergic agonist. Fenoldopam is a dopamine agonist used to treat severe hypertension. Other drugs are nonselective adrenergic agonists that could cause unwanted side effects.
Which of the following is correct regarding carvedilol? A. Carvedilol is a cardioselective β-blocker. B. Carvedilol is safe for use in asthma patients. C. Carvedilol has α1 -blocking activity D. Carvedilol is contraindicated in the treatment of stable chronic heart failure.
Correct answer = C. Carvedilol is a nonselective β-blocker with α1-blocking activity. Since it also blocks β2 receptors in the lungs, carvedilol could exacerbate asthma. Carvedilol is not used in patients with acute exacerbation of heart failure but is used in the treatment of stable, chronic heart failure.
Which of the following adrenergic agonists is commonly present in nasal sprays available over-the-counter (OTC) to treat nasal congestion? A. Clonidine. B. Albuterol. C. Oxymetazoline. D. Dobutamine. E. Norepinephrine.
Correct answer = C. Drugs with selective α1 agonistic activ- ity are commonly used as nasal decongestants because of their ability to cause vasoconstriction in the nasal vessels. Oxymetazoline is an α1 agonist and therefore the preferred drug among the choices as a nasal decongestant. Clonidine is an α2 agonist, albuterol is a β2 agonist, dobutamine is a β1 agonist, and norepinephrine is a nonselective adrenergic agonist.
Which of the following is correct regarding adrenergic neurotransmission? A. Epinephrine is the major neurotransmitter released from sympathetic nerve terminals. B. Norepinephrine is mainly released from the adrenal glands. C. Tricyclic antidepressants and cocaine prevent reuptake of norepinephrine into the nerve terminals. D. Monoamine oxidase (MAO) converts dopamine to norepinephrine in the nerve terminal.
Correct answer = C. Tricyclic antidepressants (TCAs) and cocaine inhibit the transporter protein that prevents the reuptake of norepinephrine into the sympathetic nerve terminals. Norepinephrine, not epinephrine, is the major neurotransmitter released from sympathetic nerve terminals. Epinephrine, not norepinephrine, is mainly released from the adrenal glands. Dopamine is converted to norepinephrine by dopamine β-hydroxylase, not by MAO.
60-year-old female patient started on a new antihypertensive medication recently. Her blood pressure seems to be under control, but she complains of fatigue, drowsiness, and fainting when she gets up from the bed (orthostatic hypotension). Which of the following drugs is she most likely taking? A. Metoprolol. B. Propranolol. C. Prazosin. D. Clonidine.
Correct answer = C. α-Blockers (prazosin) are more likely to cause orthostatic hypotension compared to β-blockers (metoprolol, propranolol) and α2 agonists (clonidine).
open Na+ channels
How do nicotinic receptors work?
One of your patients who is hypertensive and gets mild asthma attacks occasionally bought an herbal remedy online to help with his asthma. He is not on any asthma medications currently but is receiving a β1-selective blocker for his hypertension. The herbal remedy seems to relieve his asthma attacks, but his blood pressure seems to increase despite the β-blocker therapy. Which of the following drugs is most likely present in the herbal remedy he is taking? A. Phenylephrine. B. Norepinephrine. C. Dobutamine. D. Ephedrine. E. Salmeterol.
Correct answer = D. Two drugs among the choices that could relieve asthma are ephedrine and salmeterol, as they activate β2 receptors in the bronchioles and cause bronchodilation. However, salmeterol is a selective β2 agonist and should not cause an increase in blood pressure. Ephedrine on the other hand stimulates the release of norepinephrine and acts as a direct agonist at α- and β-adrenergic receptors, thus causing an increase in blood pressure. Phenylephrine (a nonselective α agonist) does not cause bronchodilation. Norepinephrine is a nonselective adrenergic agonist that does not have any stimulatory effects on β2 receptors. Also, norepinephrine is not active when given orally.
A 12-year-old boy who is allergic to peanuts was brought to the emergency room after accidentally consuming peanuts contained in fast food. He is in anaphylactic shock. Which of the following drugs would be most appropriate to treat this patient? A. Norepinephrine. B. Phenylephrine. C. Dobutamine. D. Epinephrine.
Correct answer = D. Norepinephrine has more α agonis- tic effects and activates mainly α1, α2, and β1 receptors. Epinephrine has more β agonistic effects and activates mainly α1, α2, β1, and β2 receptors. Phenylephrine has pre- dominantly α effects and activates mainly α1 receptors. Dobutamine mainly activates β1 receptors and has no signif- icant effects on β2 receptors. Thus, epinephrine is the drug of choice in anaphylactic shock that can both stimulate the heart (β1 activation) and dilate bronchioles (β2 activation).
A 70-year-old male needs to be treated with an α-blocker for overflow incontinence due to his enlarged prostate. Which of the following drugs would you suggest in this patent that will not affect his blood pressure significantly? A. Prazosin. B. Doxazosin. C. Phentolamine. D. Tamsulosin. E. Terazosin.
Correct answer = D. Tamsulosin is an α1 antagonist that is more selective to the α1 receptor subtype (α1A) present in the prostate and less selective to the α1 receptor subtype (α1B) present in the blood vessels. Therefore, tamsulosin does not affect blood pressure significantly. Prazosin, doxa- zosin, terazosin, and phentolamine antagonize both these subtypes and cause significant hypotension as a side effect.
All of the following are correct regarding adrenergic receptors, except: A. α1 Receptors are primarily located on the postsynaptic membrane in the effector organs. B. α Receptors are primarily located on the 2 presynaptic sympathetic nerve terminals. C. β1 Receptors are found mainly in the heart. D. β2 Receptors are found mainly in adipose tissue.
Correct answer = D. α1 Receptors are located on the post- synaptic membrane in the effector organs such as blood vessels. α2 Receptors are mainly found on the presynaptic sympathetic nerve terminals, where they inhibit the release of norepinephrine when activated. β1 Receptors are found in the heart, in addition to some other tissues, and cause increase in heart rate and contractility when activated. β2 receptors are found in the lungs, in addition to some other tissues, and cause relaxation of bronchial smooth muscles when activated. β3 Receptors are found in adipose tissue and are involved in lipolysis.
Which of the following adrenergic agonists is most likely to cause CNS side effects when administered systemically? A. Epinephrine. B. Norepinephrine. C. Isoproterenol. D. Dopamine. E. Ephedrine.
Correct answer = E. Ephedrine is more lipophilic compared to the other drugs listed and therefore is more likely to cross the blood-brain barrier when administered systemi- cally. Therefore, ephedrine is more likely to cause CNS side effects compared to other listed drugs.
new antihypertensive drug was tested in an animal model of hypertension. The drug when given alone reduces blood pressure in the animal. Norepinephrine when given in the presence of this drug did not cause any significant change in blood pressure or heart rate in the animal. The new drug is similar to which of the following drugs in terms of its pharmacological mechanism of action? A. Prazosin. B. Clonidine. C. Propranolol. D. Metoprolol. E. Carvedilol.
Correct answer = E. Norepinephrine activates both α1 and β1 receptors and causes an increase in heart rate and blood pressure. A drug that prevents the increase in blood pressure caused by norepinephrine should be simi- lar to carvedilol that antagonizes both α1 and β1 receptors. Prazosin is an α1 antagonist, clonidine is an α2 agonist, and propranolol and metoprolol are β antagonists, and these drugs cannot completely prevent the cardiovascular effects of norepinephrine.
Pilocarpine
DOC for acute angle glaucoma
Blocking of sympathetic response
Decreased HR is caused by
Correct answer = E. Based on the information presented here, since morphine is more efficacious than is ibupro- fen, it is going to provide more pain relief. As long as the situation warrants the necessity of such efficacious pain relief and without any information about differences in side effects caused by the two drugs, morphine is the better choice. Choice C would only be true if both drugs bound to the same receptor population, and that is not the case. The other choices are incorrect statements.
If 10 mg of morphine produces a greater analgesic response than can be achieved by ibuprofen at any dose, which of the following statements is correct? A. Morphine is less efficacious than is ibuprofen. B. Morphine is less potent than is ibuprofen. C. Morphine is a full agonist, and ibuprofen is a partial agonist. D. Ibuprofen is a competitive antagonist. E. Morphine is a better drug to take for pain relief than is ibuprofen.
Correct answer = B. Without information about the maximal effect of these drugs, no conclusions can be made about efficacy or intrinsic activity. E is false because the maximal response obtained is often more important than the amount of drug needed to achieve it.
If 10 mg of naproxen produces the same analgesic response as 100 mg of ibuprofen, which of the following statements is correct? A. Naproxen is more efficacious than is ibuprofen. B. Naproxen is more potent than ibuprofen. C. Naproxen is a full agonist, and ibuprofen is a partial agonist. D. Naproxen is a competitive antagonist. E. Naproxen is a better drug to take for pain relief than is ibuprofen.
Correct answer = B. Muscarinic agonists (for example, ACh, pilocarpine) contract the circular smooth muscles in the iris sphincter and constrict the pupil (miosis). Anticholinesterases (for example, neostigmine, physostig- mine) also cause miosis by increasing the level of ACh. Muscarinic antagonists, on the other hand, relax the circu- lar smooth muscles in the iris sphincter and cause dilation of the pupil (mydriasis)
If an ophthalmologist wants to dilate the pupils for an eye examination, which of the following drugs/classes of drugs could be theoretically useful? A. Muscarinic receptor activator (agonist). B. Muscarinic receptor inhibitor (antagonist). C. Acetylcholine. D. Pilocarpine. E. Neostigmine.
Correct answer = C. Since there is already a deficiency in brain cholinergic function in Alzheimer's disease, inhibiting cholinergic receptors or inhibiting the release of ACh will worsen the condition. Activating the acetylcholinesterase enzyme will increase the degradation of ACh, which will again worsen the condition. However, inhibiting the acetyl- cholinesterase enzyme will help to increase the levels of ACh in the brain and thereby help to relieve the symptoms of Alzheimer's disease
In Alzheimer's disease, there is a deficiency of cholinergic neuronal function in the brain. Theoretically, which of the following strategies will be useful in treating the symptoms of Alzheimer's disease? A. Inhibiting cholinergic receptors in the brain. B. Inhibiting the release of acetylcholine in the brain. C. Inhibiting the acetylcholinesterase enzyme in the brain. D. Activating the acetylcholinesterase enzyme in the brain
ACh, muscarinic
In the PNS, post-ganglionic neurons release _____, that binds to _____ receptors on effectors
Correct answer = A. Since naloxone has no effect by itself, B and C are incorrect. Since it decreases the effect of an agonist but this inhibition can be overcome by giving a higher dose of morphine, naloxone must be a competitive antagonist. No information is given about potency of either drug.
In the presence of naloxone, a higher concentration of morphine is required to elicit full pain relief. Naloxone by itself has no effect. Which of the following is correct regarding these medications? A. Naloxone is a competitive antagonist. B. Morphine is a full agonist, and naloxone is a partial agonist. C. Morphine is less efficacious than is naloxone. D. Morphine is less potent than is naloxone. E. Naloxone is a noncompetitive antagonist.
Correct answer = B. Pentazocine has a lower Emax value than does morphine but still has some efficacy. Thus, pen- tazocine is a partial agonist. Even though pentazocine blocks some of the actions of morphine, since it has some efficacy, it cannot be an antagonist. No information is given about the potency of either drug.
In the presence of pentazocine, a higher concentration of morphine is required to elicit full pain relief. Pentazocine by itself has a smaller analgesic effect than does morphine, even at the highest dose. Which of the following is correct regarding these medications? A. Pentazocine is a competitive antagonist. B. Morphine is a full agonist, and pentazocine is a partial agonist. C. Morphine is less efficacious than is pentazocine. D. Morphine is less potent than is pentazocine. E. Pentazocine is a noncompetitive antagonist
Correct answer = E. Picrotoxin has no efficacy alone, so B and C are false. Since it decreases the maximal effect of diazepam, it is a noncompetitive antagonist. No information is given about potency of either drug.
In the presence of picrotoxin, diazepam is less efficacious at causing sedation, regardless of the dose. Picrotoxin by itself has no sedative effect even at the highest dose. Which of the following is correct? A. Picrotoxin is a competitive antagonist. B. Diazepam is a full agonist, and picrotoxin is a partial agonist. C. Diazepam is less efficacious than is picrotoxin. D. Diazepam is less potent than is picrotoxin. E. Picrotoxin is a noncompetitive antagonist
Neostigmime
Reverses post-intubation neuromuscular blockers
Correct answer = A. A full agonist has an Emax similar to the endogenous ligand. A partial agonist would only produce a partial effect. An antagonist would block the effects of an endogenous agonist. An inverse agonist would reverse the constitutive activity of receptors and exert the opposite pharmacological effect
Isoproterenol produces maximal contraction of cardiac muscle in a manner similar to epinephrine. Which of the following best describes isoproterenol? A. Full agonist. B. Partial agonist. C. Competitive antagonist. D. Irreversible antagonist. E. Inverse agonist.
B. Low
KR2250 is an investigational new drug with a small molecular weight and extensive protein binding to albumin. It will have a ____________ volume of distribution. A. High B. Low C. Extremely high D. Normal
Blocks release of ACh
MOA Botulinum toxin
Atropine toxicity symptoms
Mad as a hatter, red as a beet, dry as a bone, blind as a bat, hot as a hare- confusion, dry mucous, no sweat, blurred vision, skin flushed, hyperthermia
Rocuronium is used as a paralytic
Memory trick: surgeon might ask "you ready to ROCk and roll" before surgery
blood vessels
Only sympathetic innervation
The drug would build up in the patients system causing increased ADE
Opioid analgesic Codeine is a prodrug that requires activation by CYP2D6. What would the outcome be in a patient who is a 2D6 poor metabolizer?
Atropine
Organophosphate poisoning treatment
Cisatracurium (spontaneously degrades in plasma)
Patient comes into the ER with liver and ESRF. Which neuromuscular blocker is indicated?
Benztropine or Trihexyphenidyl
Patient has recently been diagnosed with Parkinson's Disease and been prescribed Haldol as an antipsychotic. What medication would be a good adjunct to this?
Scopolamine and place the patch behind you ear before you board and patch can be reapplied every 3 days.
Patient is going on a cruise and has a history of seasickness. What medication should you prescribe and what instructions do you need to tell the patient?
Bathenicol
Prescribed for atonic bladder
ACh, nicotinic
Presynaptic ganglion for sympathetic nervous system
Correct answer = D. Activation of the parasympathetic system causes a reduction in heart rate, constriction of the pupil, an increase in gastric motility and salivation, and contraction of the bladder muscle. Therefore, inhibition of the parasympathetic system causes an increase in heart rate, dilation of the pupil, a decrease in gastric motility, dry mouth, and relaxation of detrusor muscles.
Which of the following changes could theoretically happen in a person when the parasympathetic system is inhibited using a pharmacological agent? A. Reduction in heart rate. B. Constriction of the pupil (miosis). C. Increase in gastric motility. D. Dry mouth (xerostomia). E. Contraction of detrusor muscle in the bladder.
B. Ipratropium
Which of the following is a SAMA? A. Tiotrpium B. Ipratropium C. Aclidinium
Correct answer = A. A muscarinic agonist binds to and activates muscarinic receptors in the heart, endothelial cells (blood vessels), the gut, and iris sphincter (eye) and urinary bladder wall muscles, in addition to several other tissues. Activation of muscarinic receptors by an agonist causes a reduction in heart rate, constriction of circular muscles in the iris sphincter leading to constriction of the pupil (miosis), increased GI motility (hence, diarrhea, not constipation), and contraction of bladder muscles leading to an increase (not decrease) in urination frequency. In the endothelial cells of blood vessels, muscarinic activation pro- duces release of nitric oxide that causes vasorelaxation and a reduction (not increase) in blood pressure.
Which of the following is a systemic effect of a muscarinic agonist? A. Reduced heart rate (bradycardia). B. Increased blood pressure. C. Mydriasis (dilation of the pupil). D. Reduced urinary frequency. E. Constipation.
Correct answer = A. Neurotransmitters generally bind to the membrane receptors on the postsynaptic effector cells and cause cellular effects. Acetylcholine (ACh) binds to cholin- ergic muscarinic receptors in the effector cells and activates the second messenger pathway in the effector cells, which in turn causes cellular events. These types of receptors that are coupled to second messenger systems are known as metabotropic receptors. Thus, metabotropic receptors do not directly activate ion channels. ACh also binds to cholin- ergic nicotinic receptors and activates ion channels on the effector cells directly. These types of receptors that activate ion channels directly are known as ionotropic receptors
Which of the following is correct regarding membrane receptors and signal transduction? A. ANS neurotransmitters bind to membrane receptors on the effector cells, which leads to intracellular events. B. Cholinergic muscarinic receptors are examples of ionotropic receptors. C. Cholinergic nicotinic receptors are examples of metabotropic receptors. D. Metabotropic receptors activate ion channels directly
Correct answer = A. Neurotransmitters are released from presynaptic neurons, triggered by the arrival of an action potential in the presynaptic neuron (not in the postsynap- tic cell). When an action potential arrives in the presynaptic neuron, calcium enters the presynaptic neuron and the cal- cium levels increase in the neuron before the neurotrans- mitter is released. The main neurotransmitters in the ANS are norepinephrine and acetylcholine.
Which of the following is correct regarding neurotrans- mitters and neurotransmission? A. Neurotransmitters are released from the presynaptic nerve terminals. B. Neurotransmitter release is triggered by the arrival of action potentials in the postsynaptic cell. C. Intracellular calcium levels drop in the neuron before the neurotransmitter is released. D. Serotonin and dopamine are the primary neurotransmitters in the ANS.
Correct answer = D. Somatic motor neurons innervate skel- etal muscles (not smooth muscle) and have no ganglia. Answers A and B are incorrect, since there are no ganglia. Also, the responses in the somatic motor nervous system are faster compared to the responses in the autonomic nervous system due to the lack of ganglia in the former.
Which of the following is correct regarding somatic motor neurons? A. The neurotransmitter at the somatic motor neuron ganglion is acetylcholine. B. The neurotransmitter at the somatic motor neuron ganglion is norepinephrine. C. Somatic motor neurons innervate smooth muscles. D. Somatic motor neurons do not have ganglia. E. Responses in the somatic motor neurons are generally slower than in the autonomic nervous system.
Correct answer = C. The neurotransmitter at the sympathetic and parasympathetic ganglia is acetylcholine. Sympathetic neurons release NE and parasympathetic neurons release ACh in the effector cells. Afferent neurons carry signals from the periphery to the CNS.
Which of the following is correct regarding the autonomic nervous system (ANS)? A. Afferent neurons carry signals from the CNS to the effector organs. B. The neurotransmitter at the parasympathetic ganglion is norepinephrine (NE). C. The neurotransmitter at the sympathetic ganglion is acetylcholine (ACh). D. Sympathetic neurons release ACh in the effector organs. E. Parasympathetic neurons release NE in the effector organs.
Correct answer = D. Lipid-soluble drugs readily cross the blood-brain barrier because they can dissolve easily in the membrane of endothelial cells. Ionized or polar drugs gen- erally fail to cross the blood-brain barrier because they are unable to pass through the endothelial cells, which do not have slit junctions.
Which of the following is true about the blood-brain barrier? A. Endothelial cells of the blood-brain barrier have slit junctions. B. Ionized or polar drugs can cross the blood-brain barrier easily. C. Drugs cannot cross the blood-brain barrier through specific transporters. D. Lipid-soluble drugs readily cross the blood-brain barrier. E. The capillary structure of the blood-brain barrier is similar to that of the liver and spleen.
Correct answer = A. When a person is in the "fight-or-flight" mode, as in the case of a bear attack, the sympathetic system will be activated. Activation of the sympathetic sys- tem causes an increase in heart rate and blood pressure and a decrease (not increase) in gastric motility. It also causes dilation (not constriction) of the pupil and inhibition of lacrimation.
Which of the following physiological changes could happen when a person is attacked by a grizzly bear? A. Increase in heart rate. B. Increase in lacrimation (tears). C. Constriction of the pupil (miosis). D. Increase in gastric motility.
Correct answer = C. The parasympathetic nervous sys- tem maintains essential bodily functions, such as vision, movement of food, and urination. It uses acetylcholine, not norepinephrine, as a neurotransmitter, and it discharges as discrete fibers that are activated separately. The post- ganglionic fibers of the parasympathetic system are short compared to those of the sympathetic division. The adrenal medulla is under the control of the sympathetic system.
Which of the following statements concerning the parasympathetic nervous system is correct? A. The parasympathetic system uses norepinephrine as a neurotransmitter. B. The parasympathetic system often discharges as a single, functional system. C. The parasympathetic division is involved in accommodation of near vision, movement of food, and urination. D. The postganglionic fibers of the parasympathetic division are long compared to those of the sympathetic nervous system. E. The parasympathetic system controls the secretion of the adrenal medulla.
Correct answer = A. Acetylcholine is the neurotransmitter in the cholinergic system, and it activates both muscarinic and nicotinic cholinergic receptors, not adrenergic receptors. Norepinephrine activates adrenergic receptors, not musca- rinic receptors. Activation of the sympathetic system causes an increase in blood pressure (not a drop in blood pressure) due to vasoconstriction and stimulation of the heart.
Which of the following statements is correct regarding the sympathetic and parasympathetic systems? A. Acetylcholine activates muscarinic receptors. B. Acetylcholine activates adrenergic receptors. C. Norepinephrine activates muscarinic receptors. D. Activation of the sympathetic system causes a drop in blood pressure.
Correct answer = C. One explanation for the existence of spare receptors is that any one agonist-receptor bind- ing event can lead to the activation of many more cellular response elements. Thus, only a small fraction of the total receptors need to be bound to elicit a maximum cellular response. The other choices do not accurately describe spare receptor systems.
Which of the following statements most accurately describes a system having spare receptors? A. The number of spare receptors determines the maximum effect. B. Spare receptors are sequestered in the cytosol. C. A single drug-receptor interaction results in many cellular response elements being activated. D. Spare receptors are active even in the absence of an agonist. E. Agonist affinity for spare receptors is less than their affinity for "non-spare" receptors.
Correct answer = C. Highly hydrophilic drugs have poor oral bioavailability, because they are poorly absorbed due to their inability to cross the lipid-rich cell membranes. Highly lipo- philic (hydrophobic) drugs also have poor oral bioavailability, because they are poorly absorbed due their insolubility in aqueous stomach fluids and therefore cannot gain access to the surface of cells. Therefore, drugs that are largely hydro- phobic, yet have aqueous solubility have greater oral bio- availability because they are readily absorbed.
Which of the following types of drugs will have maximum oral bioavailability? A. Drugs with high first-pass metabolism. B. Highly hydrophilic drugs. C. Largely hydrophobic, yet soluble in aqueous solutions. D. Chemically unstable drugs. E. Drugs that are P-glycoprotein substrates
Correct answer = E. Up-regulation of receptors occurs when receptor activation is lower than normal, such as when the receptor is continuously exposed to an antago- nist for that receptor. Down-regulation of receptor number occurs when receptor activation is greater than normal because of continuous exposure to an agonist
Which of the following would up-regulate postsynaptic β1 adrenergic receptors? A. Daily use of amphetamine that causes norepinephrine to be released. B. A disease that causes an increase in the activity of norepinephrine neurons. C. Daily use of isoproterenol, a β1 receptor agonist. D. Daily use of formoterol, a β2 receptor agonist. E. Daily use of propranolol, a β1 receptor antagonist.
ONLY a paralysis, NO anesthetic capabilities
Why aren't neuromuscular blockers sufficient on their own when performing surgery?
vasoconstriction
alpha 1 response
