Annual Review of Pharmacology and Toxicology Volume 45, (Annual Review of Pharmacology and Toxicology). Read more. Editorial Reviews. About the Author. About the Author Jessica Gleason, MD is resident at the .. Download Audiobooks · Book Depository Books With Free Delivery Worldwide · Box Office Mojo Find Movie Box Office Data · ComiXology. Thousands of. Here you can directly get it ⇩ ⇰ File formats: ePub, PDF, site, Audiobook, mobi , ZIP. * Download ~>> Deja Review Pharmacology, Second Edition 2nd Edition.

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Chloroquine more potent and less toxic than quinine What drugs are effective against the exoerythrocytic forms of malaria? Primaquine Is primaquine effective against erythrocytic forms of malaria?

No Give examples of antimalarial drugs that are effective against the erythrocytic forms of malaria: To prevent recurrence of infection, hepatic forms of these parasites must be eliminated. What are the adverse effects of primaquine?

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Hemolytic anemia in patients with G6PD deficiency; methemoglobinemia; agranulocytosis What is the drug of choice for acute attacks of malaria caused by chloroquine-sensitive strains of P. Chloroquine Does chloroquine have a large or small Vd?

Large What is the mechanism of action of chloroquine? It concentrates within parasite food vacuoles and raises pH leading to inhibition of growth; inhibits hemoglobin metabolism and utilization by parasites; concentrates within parasite vacuoles and raises pH leading to inhibition of growth; binds to ferriprotoporphyrin IX leading to membrane damage; inhibits DNA and RNA polymerase What continents contain the largest repositories of chloroquine-resistant P.

Porphyria; psoriasis What are the major adverse effects of quinine?

Cinchonism nausea, vomiting, diarrhea, tinnitus, vertigo ; hemolytic anemia; digoxin toxicity What other medication can cause cinchonism?

Quinidine Is quinine acidic or basic? Basic How can the urinary excretion of quinine or chloroquine be enhanced? Acidification of the urine Name two newer antimalarials that are chemically related to quinine: Halofantrine 2.

Lumefantrine What can be used to acidify the urine? Ammonium chloride What is the mechanism of action of pyrimethamine? Inhibits nucleic acid and protein metabolism in the parasites; plasmodial dihydrofolate reductase DHFR inhibitor The antimalarial effects of pyrimethamine can be potentiated by combining it with which drugs? Sulfonamides synergistic blockade of folic acid synthesis.

How is folate-deficient megaloblastic anemia reversed in patients taking pyrimethamine? Leucovorin What is the mechanism of action of leucovorin? As a reduced form of folic acid, leucovorin supplies human cells with the necessary cofactor blocked by DHFR inhibitors. What kind of compounds are the antimalarial drug artemisinin and its derivatives? Sesquiterpene lactones the active ingredient in a year-old Chinese herb—Qing Hao.

What is the antimalarial mechanism of action of artemisinin? It is thought that it is activated by heme to irreversibly decompose generating free radicals that form adducts mostly with proteins and lipids. Give examples of antimalarial drugs used in artemisinin combination therapies ACT: Sickle cell trait; G6PD deficiency Trypanosoma cruzi is responsible for causing what disease? American trypanosomiasis Chagas disease T. African trypanosomiasis sleeping sickness What drug is used as a suppressive agent in patients with acute T.

Nifurtimox What is the mechanism of action of nifurtimox? Forms intracellular oxygen-free radicals which are toxic to the parasite because of its lack of catalase oxygen radical scavenger What drug is used to treat African sleeping sickness with CNS involvement?

Eflornithine for West African trypanosomiasis; melarsoprol for East African trypanosomiasis What are the adverse events of melarsoprol? Hypersensitivity; abdominal pain; vomiting; hemolytic anemia in patients with G6PD deficiency; encephalopathy What two drugs are used in the early stages of African sleeping sickness? Pentamidine first choice for West African sleeping sickness 2. Therefore it cannot be used for late trypanosomiasis with CNS involvement.

What are the two routes of administration of pentamidine? Aerosol What fungus is pentamidine commonly used to treat? Pneumocystis carinii What drug combination is used for prophylaxis against P.

Trimethoprim-sulfamethoxazole What is the treatment of choice for T. Ingestion of undercooked, infected meat; contact with infected cats Can pregnant mothers transmit T. Visceral 2. Mucocutaneous What is the drug of choice for treating leishmaniasis? Roundworms What is another name for the trematodes? Flukes What is another name for the cestodes? Tapeworms What drug is commonly used to treat trematode infections? Praziquantel What is the mechanism of action of praziquantel?

Increases cell permeability to calcium, thereby increasing contractions with subsequent paralysis of musculature What is the mechanism of action of mebendazole? It irreversibly blocks glucose uptake; inhibits microtubule polymerization What are the adverse effects of mebendazole? Diarrhea; abdominal pain; contraindicated during pregnancy What is the mechanism of action of albendazole?

It interferes with microtubule polymerization; inhibits adenosine triphosphate ATP production thereby depleting energy availability What is the mechanism of action of thiabendazole?

Inhibits helminth-specific mitochondrial fumarate reductase What types of cutaneous adverse effects are caused by thiabendazole? Stevens-Johnson syndrome; erythema multiforme What is the mechanism of action of pyrantel? Depolarizing neuromuscular blocker thereby causing paralysis of musculature What types of helminths are affected by praziquantel?

Trematodes; cestodes What types of helminths are affected by mebendazole? Nematodes What types of helminths are affected by pyrantel? Nematodes What is the drug of choice for treating Enterobius vermicularis? Mebendazole What is the common name for E. Ivermectin What is the mechanism of action of ivermectin? Acts at helminthic gamma-aminobutyric acid GABA receptors, thereby enhancing influx of chloride and causing hyperpolarization and paralysis Why does onchocerciasis potentially lead to blindness?

A bacteria Wolbachia sp. What is another name for onchocerciasis? River blindness What drug is commonly used to treat cestode infections? Niclosamide What is the mechanism of action of niclosamide? Inhibits mitochondrial phosphorylation of ADP to ATP, thereby depleting energy availability Is niclosamide active against the ova of cestodes?

Moreover, she is very conscious as to maintain fitness in keeping with her required scuba licensing; thus, she regularly takes calcium tablets with her meals. She is diagnosed with a Mycobacterium marinum infection and begins treatment with minocycline. However, 6 weeks after treatment her condition has not resolved and she has developed new granulomas. What is the most likely reason for treatment failure in this patient? Her unique occupation gives the patient exposure to microorganisms that are uncommonly causes of infection in the lay human population.

In terms of her medications, even supplements have significant side effects and drug interactions, and must be asked about as part of your history. Calcium salts such as those used to increase calcium intake in menopausal women will chelate tetracyclines like minocycline, decreasing their oral bioavailability.

Therefore, this patient should have been instructed not to take her calcium supplement tablets 2 hours before or after a dose of her antibiotic. A year-old man is brought to the intensive care unit ICU after being found unresponsive on the floor of his home. It is unknown how long the patient had remained immobile on the floor. Respiratory effort was diminished and the patient was intubated and placed on a ventilator.

The intern on call placed the patient on a tobramycin nebulizer to suppress ventilator-associated pneumonia. The next morning, the attending physician sees this and immediately terminates this treatment. Why is tobramycin contraindicated in this patient? Aminoglycosides, such as tobramycin, are nephrotoxic and will cause further damage to the kidneys. All aminoglycosides should be used with caution in the elderly. Another consideration is ototoxicity.

Since this patient is unresponsive, we are unaware of his baseline hearing status.

A small amount of damage in an individual who is already hard of hearing could have dramatic consequences. A year-old female medical student participates in an exchange program in rural South Korea.

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Despite chemoprophylaxis mefloquine , she develops cyclic shaking chills and fever and is diagnosed with malaria. Treatment is begun with chloroquine, but the student fails to respond. Resistance to chloroquine is suspected, and the treatment is switched to quinidine plus a tetracycline with complete resolution of her symptoms. Two months after her return to the United States, she has a reoccurrence of the malarial symptoms. Why has this therapy failed to resolve her illness? The student has most likely contracted P.

Chloroquine and mefloquine resistance is an increasing problem worldwide. A quinidine plus tetracycline eg, doxycycline combination is an effective treatment regimen for eradication of chloroquine-resistant malaria. However, it is important to remember that P. Reactivation of these hypnozoites can lead to recurrence of infection months to years later.

Once the original acute attack P. Licensing exams will not expect you to determine whether a specific geographic area is endemic with chloroquine resistant strains of malaria.

You should know treatment alternatives for drug-resistant strains, as well as when addition of primaquine is necessary to eradicate hepatic repositories of the malaria parasite ie, therapy is specie-specific. During the second week of a trip to Belize, a traveler experienced some diarrhea, which was sufficient to remind him of previous admonitions about consuming food dispensed by street vendors.

Fortunately, his symptoms seem to subside and he recovered in a few days. About a month after his return, the traveler developed severe pain in the right upper quadrant of his abdomen.

When the abdominal pain persisted, he went to a gastroenterologist. The gastroenterologist performed an x-ray study of the intestine after a barium enema, a CT scan, and a serological test for E.

The results of these tests revealed pseudopolyps consistent with inflammatory bowel disease, the CT scan showed abscesses in the liver and a hemagglutination titer of 1: What antiprotozoal drug should be given to this patient? The drug of choice for this active amebic infection picture is metronidazole. It is absorbed rapidly from oral doses with a half-life in serum of about 8 hours.

It has potent activity against E. The drug is well tolerated and adverse effects are not common, but nausea, headaches, and dry mouth can occur. First-order kinetics With first-order kinetics, is it a fixed amount or fixed percentage of tumor cells that are killed by cancer chemotherapeutic agents? Fixed percentage If a chemotherapy treatment leads to a 4 log-kill reduction, then how many tumor cells would remain if there were tumor cells to begin with?

G0 Cells are not actively dividing resting state. G1 Enzymes and proteins required for DNA replication are synthesized. M Mitosis occurs. The ratio of proliferating malignant cells to nonprolifcrating G0 cells is also known as what? Growth fraction Are tumor cells more susceptible to cancer chemotherapeutic agents when they are actively dividing or when they are dormant? Actively dividing.

Thus, tumor cells which are dormant may not be sufficiently susceptible to the effects of cancer chemotherapeutic agents. What is the definition of a cell-cycle specific CCS cancer chemotherapeutic agent?

Bone marrow cells; GI mucosal cells; hair cells. Thus, the common side effects of chemotherapy include myelosuppression, GI disturbances, and alopecia. P-glycoprotein is an ATP-dependent membrane efflux transporter that is responsible for what? Pumping drugs out of cells responsible for multidrug resistance of chemotherapeutic agents Give examples of cancer chemotherapeutic agents that are commonly associated with each of the following adverse effects: Cardiotoxicity; dilated cardiomyopathy Doxorubicin Pulmonary fibrosis; pneumonitis Bleomycin Stomatitis; esophagitis Methotrexate; 5-fluorouracil; dactinomycin Hemorrhagic cystitis Cyclophosphamide; ifosfamide Hemorrhagic diathesis Peripheral neuropathy; neurotoxicity Plicamycin Nephrotoxicity Vincristine Allergic reactions Cisplatin Hepatotoxicity Etoposide; L-asparaginase Pancreatitis 6-Mercaptopurine; busulfan; Cyclophosphamide Cutaneous toxicity hand-foot syndrome L-Asparaginase 5-Fluorouracil Disulfiram-type reactions Procarbazine What is the name of the antidote that binds to and inactivates the toxic metabolites responsible for cisplatin-induced nephrotoxicity?

Amifostine What is the name of the cyclophosphamide and ifosfamide urotoxic metabolite that is responsible for causing hemorrhagic cystitis? Acrolein What is the name of the antidote that binds to and inactivates acrolein, thereby preventing hemorrhagic cystitis in patients receiving cyclophosphamide or ifosfamide chemotherapy? Dexrazoxane Give examples of antimetabolite cancer chemotherapeutic agents: Methotrexate; 5-fluorouracil; cytarabine; fludarabine; 6-thioguanine; 6-mercaptopurine Are the antimetabolite cancer chemotherapeutic agents CCS?

Leucovorin, which acts as an active form of folic acid replenishing the folate pool that has bypassed the inhibited DHFR and is more readily taken up by normal cells than by malignant cells What are the adverse effects of methotrexate?

Stomatitis; bone marrow suppression BMS ; urticaria; alopecia; nausea; vomiting; diarrhea; nephrotoxicity; hepatotoxicity; pulmonary toxicity; neurotoxicity What is the mechanism of action of 5-fluorouracil?

Pyrimidine analog that is converted to active 5-FdUMP which inhibits thymidylate synthetase, thereby decreasing the amount of cellular thymidine and subsequent DNA What is the mechanism of action of cytarabine? Pyrimidine antagonist What is the mechanism of action of both 6-mercaptopurine and 6-thioguanine? Purine antagonists What immunosuppressive drug becomes active only after being converted to 6- mercaptopurine?

Azathioprine Because 6-mercaptopurine is metabolized by xanthine oxidase, its serum levels may be significantly increased when given concomitantly with what other medication?

Allopurinol xanthine oxidase inhibitor What enzyme activates 6-mercaptopurine to its corresponding nucleotide form by adding a ribose phosphate to its structure?

Nausea; vomiting; diarrhea; hepatotoxicity; BMS Give examples of antitumor antibiotics: Doxorubicin; daunorubicin; dactinomycin; plicamycin; bleomycin; idarubicin Are the antitumor antibiotics CCS? Yes S-phase Name three anthracycline antitumor antibiotics: Doxorubicin 2. Daunorubicin 3. Idarubicin What is the mechanism of action of the anthracycline antibiotics?

Dactinomycin 2. Bleomycin 3. Mitomycin What is the mechanism of action of bleomycin?

Complexes with iron and reacts with oxygen which in turn leads to DNA strand scission Which phase of the cell cycle is bleomycin specific for? G2 Give examples of anticancer alkylating agents: Cyclophosphamide; ifosfamide; mechlorethamine; nitrosoureas carmustine, lomustine, streptozotocin ; cisplatin; carboplatin Are the anticancer alkylating chemotherapeutic agents CCS?

No What is the mechanism of action of anticancer alkylating agents? Covalently bind alkylation to DNA leading to cross-linked and dysfunctional DNA strands Give examples of anticancer mitotic inhibitors: Paclitaxel; docetaxel; vincristine; vinblastine; vinorelbine Are the anticancer mitotic inhibitors CCS?

Yes M phase What is the mechanism of action of vincristine and vinblastine? They are vinca alkaloids that inhibits the ability of tubulin to polymerize, thereby preventing formation of the microtubule structures needed during mitosis.

What adverse effects do vincristine and vinblastine have in common? Nausea; vomiting; diarrhea; alopecia; phlebitis; cellulites Are vincristine and vinblastine vesicants?

Yes, they are strong vesicants. Which adverse effect is unique to vincristine? Peripheral neuropathy Which adverse effect is unique to vinblastine? BMS What plant are the vinca alkaloids derived from? Periwinkle plant Which plant is paclitaxel a derivative of?

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Needles of the Western or Pacific yew tree What is the mechanism of action of paclitaxel? Binds to tubulin and increases polymerization and stabilization of the microtubule structure, thereby preventing depolymerization What are the adverse effects of paclitaxel?

Neutropenia; alopecia; hypersensitivity reactions How are hypersensitivity reactions prevented in patients receiving paclitaxel cancer chemotherapy? Etoposide 2. Teniposide What is the mechanism of action of the epipodophyllotoxin cancer chemotherapeutic agents? Topotecan 2. Irinotecan What is the mechanism of action of L-asparaginase? Hydrolyzes asparagine to aspartic acid and ammonia, thereby depriving tumor cells of asparagine required for protein synthesis This short chapter is meant as an overview of basic concepts of cancer chemotherapy.

Clinical pharmacological therapies for specific cancer subtypes are discussed later in the text in relevant chapters. It is divided into the sympathetic and the parasympathetic nervous systems. What is the major neurotransmitter of the parasympathetic autonomic nervous system? Acetylcholine ACh. ACh is released into the synaptic clefts from the pre-and the postsynaptic neurons of the parasympathetic nervous system.

In the sympathetic nervous system, what neurotransmitter is released from the preganglionic neuron into the synaptic cleft? Remember that while the postganglionic neurotransmitters may differ between the sympathetic and parasympathetic branches of the autonomic nervous system, the preganglionic neurotransmitter released into the synaptic cleft is identical—ACh.

Where are sympathetic preganglionic fibers located? In the paravertebral chains on either side of the spinal column or the prevertebral ganglia on the ventral surface of the aorta.

Sympathetic preganglionic fibers are short. Where are parasympathetic preganglionic fibers located? In or near the wall of the organ they innervate. Parasympathetic preganglionic fibers are very long. Where are nicotinic receptors located? It decreases the heart rate. Remember that at rest the heart is constantly under parasympathetic tone to slow the heart rate from the intrinsic rate set by the sinoatrial SA node at about 80 beats per minute.

What enzyme catalyzes the reaction between choline and acetyl-CoA to form ACh? Botulinum toxin What organism produces botulinum toxin? Clostridium botulinum anaerobic, spore forming, gram-positive rod The venom of which spiders result in the release of stored ACh into the synapse? Any spider of the genus Latrodectus widow spiders of which the black widow is the most common species found in North America.

What enzyme degrades ACh? Choline and acetate Where is AChE located in the autonomic nervous system? In the synaptic cleft What is muscarine? It is an alkaloid found in various poisonous mushrooms. Where are each of the following types of muscarinic receptors found in the body? M1 Nerves; gastric parietal cells M2 Nerves; cardiac cells; smooth muscle M3 Smooth muscle; exocrine glands; lungs; gastrointestinal GI tract; eye; bladder M4 CNS M5 CNS For each of the following muscarinic receptor types, name the type of G-protein it is coupled to and the second messenger system responsible for execution of its activity upon stimulation: Vascular tone is primarily determined by the degree of stimulation of adrenergic receptors of the sympathetic nervous system which directly innervate the vascular smooth muscle cells.

However, there are muscarinic receptors located on the vasculature. How can ACh lower blood pressure? ACh binds to ACh receptors in the vasculature leading to increased synthesis of nitric oxide NO via second messenger pathways.

An increase in NO leads to vasodilation. NO is also known as what?

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Yes Does ACh increase or decrease the following in other words, what is the effect of parasympathetic stimulation of the following? Blood pressure Decreases both arterial and venous dilation via NO Heart rate Decreases via M2 receptors Salivation Increases via M3 receptors Lacrimation Increases via M3 receptors Sweating Increases via sympathetic stimulation of muscarinic cholinergic receptors GI secretions Increases via M3 receptors GI motility Increases via M3 receptors Miosis constriction of pupil Increases via M3 receptors Bladder detrusor muscle tone Increases via M3 receptors Bladder sphincter tone Decreases in combination with increased detrusor tone this leads to increased urination also via M3receptors Bronchodilation Decreases via M3 receptors What does ACh do to the ciliary muscle of the eye?

Increased contraction which leads to increased accommodation How does ACh cause miosis? Increased contraction of the circular muscle in the iris Does bethanechol have muscarinic activity? Yes agonist Does bethanechol have nicotinic activity? No Does AChE have a high affinity for bethanechol? No zero affinity. This gives bethanechol a long duration of action.

What is a clinical use for bethanechol? Nonobstructive urinary retention as can result from denervation of the urinary sphincter in conditions such as diabetes or spinal cord injury. Bethanechol can also be used for gastroesophageal reflux disease GERD. As a cholinergic drug, it will increase detrusor tone and GI motility. Does carbachol have muscarinic activity? Yes, it is a muscarinic agonist. Does carbachol have nicotinic activity? Yes, it is also a nicotinic agonist. Does AChE have a high affinity for carbachol?

No, the enzyme has zero affinity for carbachol. What is carbachol used for? It is a miotic agent to reduce intraocular pressure IOP in emergency settings of narrow- angle and open-angle glaucoma. Does pilocarpine have muscarinic activity?

Does pilocarpine have nicotinic activity? No Does AChE have a high affinity for pilocarpine? No, the enzyme has zero affinity for pilocarpine. What is pilocarpine used for? It is the miotic drug of choice to lower IOP in emergency settings of narrow-angle and open- angle glaucoma. Can pilocarpine cross the blood-brain barrier BBB?

Because it is a tertiary, uncharged amine. Give examples of reversible AChE inhibitors: Neostigmine; pyridostigmine; physostigmine; edrophonium; rivastigmine; donepezil; galantamine; tacrine What are donepezil, galantamine, rivastigmine, and tacrine used for? Alzheimer-type dementia. Neostigmine 2. Pyridostigmine As a result, these drugs will not reverse the central nervous system effects of cholinergic toxicity.

What short-acting AChE inhibitor is used to diagnose myasthenia gravis and is also used to differentiate myasthenic from cholinergic crisis? The trade name of edrophonium is Tensilon. This test is commonly referred to as the Tensilon test. Which reversible AChE inhibitor is used as an antidote in atropine overdose? Give examples of irreversible AChE inhibitors: Echothiophate; isoflurophate; sarin; malathion; parathion Name an irreversible AChE inhibitor that is used as nerve gas: Sarin Which two AChE inhibitors are used as insecticides?

Malathion 2. Parathion What is another name for the irreversible AChE inhibitors? Organophosphates How do organophosphates irreversibly inhibit AChE?

The phosphate group covalently binds to serine hydroxyl group in the active site of AChE, thereby rendering the enzyme permanently inactive. What is used to counteract the muscarinic and CNS effects of organophosphate poisoning? Atropine via competitive inhibition. Atropine binds the muscarinic receptors, outcompeting the increased levels of ACh thereby preventing overstimulation.

What agent is used to reactivate inhibited AChE during organophosphate poisoning? Pralidoxime 2-PAM. It is critical to initiate treatment with pralidoxime early along with atropine to prevent the process of aging where AChE is irreversibly inactivated by the organophosphates. What are the signs and symptoms of organophosphate poisoning? Basically, parasympathetic overstimulation.

Does atropine block nicotinic receptors, muscarinic receptors, or both? It blocks muscarinic receptors. What are the pharmacologic actions of atropine?

Mydriasis; cycloplegia; tachycardia; sedation; urinary retention; constipation; dry mouth; dry eyes; decreased sweating; hallucinations; sedation; hyperthermia; delirium; blurred vision; coma high doses. What class of drugs can be used to counteract atropine overdose?

AChE inhibitors Name three drug classes that may cause antimuscarinic adverse effects: Tricyclic antidepressants TCAs 3. Increases heart rate parasympatholytic effect What is belladonna? Other toxins include scopolamine and hyoscyamine. The name belladonna derives from the cosmetic enhancing effects of dilated pupils, blushing of the cheeks, and reddening of the lips for which the plant was originally used.

How does scopolamine differ from atropine? Scopolamine has a longer duration of action, more potent CNS effects, and is able to block short-term memory. What is the main therapeutic indication of scopolamine? Motion sickness Giving drugs with anticholinergic activity can precipitate an emergent situation in patients with what medical condition?

Patients with narrow-angle glaucoma What are the signs and symptoms of acute-angle-closure glaucoma? General distress; pain; headache; red eye; photophobia; increased IOP; visual changes; malaise; nausea; vomiting What two anticholinergic agents are quaternary ammonium compounds and used for the treatment of asthma and chronic obstructive pulmonary disease COPD? Ipratropium 2. Tiotropium Tiotropium has a longer half-life compared to ipratropium.

Does ipratropium effect airway secretions? No unlike atropine, which decreases airway secretions Name three ganglionic blocking agents: Hexamethonium 2. Mecamylamine 3. Trimethaphan What are ganglionic blocking agents primarily used for? Lowering blood pressure; blocking autonomic nervous system reflexes; smoking cessation due to blockade of central nicotine receptors Why can ganglionic blockers cause a marked postural hypotension?

Since sympathetic tone to the blood vessels is blocked, both arterial and venous dilation occur, lowering blood pressure. Moreover, the ganglionic blockers prevent the sympathetically mediated baroreceptor response to a sudden decrease in blood pressure, such as that occurs with a rapid change in position from sitting to standing.

Neuromuscular blocking agents NMBs can be grouped into what two general categories? Depolarizing 2. Nicotinic receptors remember the NMJ has nicotinic receptors.

How many subunits is the nicotinic receptor made of? Five subunits. Which subunit of the nicotinic receptor does ACh bind to? Sodium channel What is the most commonly used NMB?

Succinylcholine, the only depolarizing NMB. This is an ideal drug for endotracheal intubation due to its fast onset of action and short duration of action. How does succinylcholine work at the NMJ? It behaves as a cholinergic agonist that remains bound to the ACh receptor for a prolonged period. What happens during each of the following phases of succinylcholine activity at the NMJ? Phase I The receptor becomes depolarized and transient fasciculations are observed as various motor units depolarize.

Phase II The receptor becomes resistant to depolarization and a flaccid paralysis ensues. What are the two main uses of succinylcholine? It is used for facilitation of endotracheal intubation via relaxation of pharyngeal and laryngeal muscles. It is used as an adjunct during electroconvulsive shock therapy to prevent prolonged full body convulsions which would result in muscle breakdown.

A tourniquet is placed on a lower extremity to prevent the drug from reaching this location so that the seizure is visible in a localized area and the rest of the body is spared. Is succinylcholine short or long acting? It is short acting with a duration of minutes because of rapid hydrolysis by plasma cholinesterase. What are the adverse effects of succinylcholine? Malignant hyperthermia; apnea; hypertension; hyperkalemia What are the signs and symptoms of malignant hyperthermia?

Muscular rigidity; increased oxygen consumption; increased carbon dioxide production usually the first sign detected during surgery ; tachycardia; hyperthermia is a late finding How is malignant hyperthermia treated? With dantrolene What is the mechanism of action of dantrolene?

It inhibits calcium release from the sarcoplasmic reticulum of muscle cells, thereby relaxing muscle tone and reducing heat production. Succinylcholine may have a prolonged half-life in what type of patients? Patients with a genetic deficiency or altered form of plasma cholinesterase What is the mechanism of action of nondepolarizing NMBs? Tubocurarine What antidote is used in tubocurarine overdose?

Small muscles of the face and eye 2. Fingers 3. Limbs, neck, trunk 4. Intercostals 5. Diaphragm Which antimicrobial class of drugs may act in synergy with nondepolarizing NMBs by inhibiting release of ACh from nerve endings by competing with calcium ions, thereby increasing neuromuscular blockade?

Aminoglycosides most likely to occur with high doses; patients with hypocalcemia, hypomagnesemia, or neuromuscular disorders Give examples of nondepolarizing NMBs: Tubocurarine; atracurium; mivacurium; rocuronium; vecuronium; pancuronium; pipercuronium What is the only nondepolarizing NMB that does not require dosage reduction in patients with renal failure?

Atracurium, which excreted in bile, not in urine What nondepolarizing NMB has the most rapid onset of action? Epinephrine; norepinephrine; dopamine What amino acid is the precursor to dopamine, epinephrine, and norepinephrine? What two enzymes metabolize norepinephrine? Monoamine oxidase MAO 2. It inhibits the transport of norepinephrine from the neuronal cytoplasm into the synaptic vesicles.

What are the common side effects of reserpine? Depression; sedation What breakdown products of norepinephrine are excreted in the urine and can be measured to help diagnose pheochromocytoma?

Vanillylmandelic acid VMA ; metanephrine; normetanephrine What are the two major classes of adrenergic receptors? Norepinephrine; epinephrine; serotonin; tyramine; dopamine What neurotransmitters does MAO type B metabolize?

Dopamine is metabolized by both the A and B type of the enzyme. How does cocaine increase norepinephrine levels in the synaptic cleft? It inhibits the reuptake of neurotransmitter back into the presynaptic neuron.

How do amphetamine, ephedrine, and tyramine increase norepinephrine levels? They act as indirect sympathomimetic agents by entering the presynaptic neuron releasing stored norepinephrine into the synaptic cleft. Smooth muscle Where are D2-receptors found?

The central effects overwhelm the local effects leading to decreased blood pressure. Hypertension; severe pain; heroin withdrawal; nicotine withdrawal; ethanol dependence; clozapine-induced sialorrhea; prevention of migraines What is dexmedetomidine used for?

It will cause insulin secretion to decrease. It will cause insulin secretion to increase. Which receptor type does epinephrine preferentially bind to at low doses? Epinephrine What is the dose of epinephrine given for anaphylaxis? Deja review: Principles of Clinical Pharmacology, Second Edition. Textbook of Receptor Pharmacology, Second Edition.

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