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Stack #216591
Pharmacology II Exam 3
| Question | Answer |
|---|---|
| What is the only NRTI that reduces perinatal HIV transmission? | Zidovudine |
| MOA of NRTIs? | Analogs of naturally occuring nucleosides competitively inhibiting viral reverse transcriptase by DNA chain termination |
| SE: lipodystrophy | zidovudine/stavudine and protease inhibitors |
| Main SE of zidovudine? | bone marrow suppression |
| Bactrim (SMX-TMP) increases plasma level concentration of? | lamivudine |
| NRTI metabolized by alcohol dehyrdrogenase? | abacavir |
| Common SE's of NRTIs? | GI upset, lactic acidosis with hepatic steotosis due to mitochondrial toxicity |
| Nucleotide Reverse Transcriptase Inhibitor | Tenofovir |
| MOA of NNRTIs | Bind directly to hydrophobic pocket of the RT protein inducing a conformational change in the active site and blocks enzyme activity |
| Common SE of NNRTIs? | rashes in the trunk and extremities |
| Drugs that induce their own metabolism? | nevirapine, efavirenz |
| HIV-1 integrase enzyme inhibitor | Raltegravir |
| Metabolized by UGT | Raltegravir |
| Most effective ART? | protease inhibitors |
| SE: buffalo hump? | protease inhibitors |
| SE: alopecia, kidney stones? | indinavir |
| SE: hyperbilirubinemia due to UGT inhibition, jaundice, heart block | atazanavir |
| SE: increase bleeding hemophilia A/B | protease inhibitors |
| NNRTI not for pregnancy? | efavirenz |
| MOA of acyclovir? | Nucleoside analog that blocks DNA synthesis by inactivation of viral DNA polymerase through direct binding and competition for dNTPs - chain termination |
| Indicated for CMV retinitis in AIDS patients | ganciclovir |
| Antiviral nucleoside analog that doesn't end in chain termination? | penciclovir |
| Indicated for acyclovir-resistant HSV and VZV strains | cidofovir |
| SE: nephrotoxicity, ocular hypotony, potential human carcinogen | cidofovir |
| SE: myelosuppression and teratogenic | ganciclovir |
| MOA of Foscarnet | Inhibits HSV DNA pol and HIV-1 RT by binding to pyrophosphate binding site of polymerase and inhibiting cleavage of pyrophosphate from dNTP; blocks viral synthesis |
| Indications of Foscarnet | nucleoside-resistant HMV, VZV and CMV; CMV retitinitis; HIV |
| MOA of Adefovir | inhibits HBV DNA polymerase |
| SE: exacerbation of hepatitis after D/C, nephrotoxicity, lactic acidosis, severe hepatomegaly | Adefovir |
| MOA of Ribavirin | interference with GTP synthesis; competitive inhibition of GTP 5' capping of viral mRNA |
| SE: hemolytic anemia, bone marrow suppression, reversible deterioration in pulmonary function, teratogenic | ribavirin |
| MOA of Amantadine & Rimantadine | Inhibit viral replication by inhibiting uncoating of the virus |
| Inhalational administration | pentamidine & zanamivir |
| MOA of Zanamivir & Oseltamivir | competitive inhibitor of influenza neuraminidase which cleaves terminal sialic acid residues |
| Indications for zanamivir/oseltamivir | influenza A & B viruses resistant to amantadine and rimantadine |
| CV effects of nitrous oxide + opioids | profound cardiac depression, a fall in BP, CO, and systemic vascular resistance |
| Triggers of malignant hyperthermia | succinylcholine, volatile anesthetic agents (desflurane sevoflurane) |
| Treatment of malignant hyperthermia | dantrolene, stop giving trigger agent, hyperventilate with O2, avoid CCBs, correct hyperkalemia and acidosis, cool core temperature |
| SE of etomidate | inhibition of steroidogenesis |
| Anesthetic that has the most specific effects in the brain | ketamine |
| Specific antagonist for benzodiazepines? | flumazenil |
| BZD with shortest duration of action | midazolam |
| The preferred form of amphotericin B? | deoxycholate |
| The preferred form of amphotericin B for renal impairment? | lipid forms |
| AmpB routes of administration? | IV or intrathecally |
| What steps do you take to prevent nephrotoxicity with AmpB? | Na+ loading prior to therapy |
| How do you prevent fever and chills with AmpB? | steroid or antipyretic |
| What do you abort the fever and chills associated with AmpB with? | meperidine |
| What drug potentiates the action of doxorubicin, an anti-cancer drug? | Amp B |
| Indications for Amp B? | C. albicans, histoplasmosis, cryptococcus, aspergillus, blastomyces |
| The preferred treatment for deep fungal infections in pregnancy? | Amp B |
| Used to treat Candidal infections of the mucosa, skin and intestinal tract? | Nystatin |
| Indications for 5-FC? | systemic mycoses and meningitis caused by Cryptococcus neoformans and Candida infections (esophaglitis) |
| SE: hematological toxicity, bone marrow depression, reversible hepatic dysfunction | 5-FC |
| MOA: inhibits the methylation of ergosterol precursors, components of the fungal cell membrane | azoles |
| Azoles: order of CYP inhibition | Voriconazole > Itraconazole = Ketoconazole >> Fluconazole |
| Indications for fluconazole? | Candidiasis, Cocciodomycosis, Cryptococcal meningitis (2nd line agent) |
| Inhibits CYP450 enzymes but not the isozyme used for androgen synthesis | fluconazole |
| Contraindicated for patients with ventricular dysfunction? | itraconazole |
| DOC for histoplasmosis (non-meningeal) | itraconazole |
| DOC for blastomycosis | itraconazole |
| SE: hepatic toxicity, rash, photosensitivity, hallucinations, visual disturbances | voriconazole |
| Voriconazole is contraindicated with? | drugs that induce CYP450 (rifampin, rifabutin, carbamazepine, long-acting barbiturates) |
| Indicated for invasive aspergillus, scedosporium, fusarium, fluconazole-resistant Candida | voriconazole |
| SE: inhibits steroid synthesis by CYP450 inhibition leading to decreased testosterone (gynecomastia, decreased libido and potency in men and menstrual irregularities in women) | ketoconazole |
| Indicated for candida lusetaniae? | fluconazole |
| Topical use only in ringworm and mucocutaneous candidiasis | miconazole |
| Topical application for mucosal and cutaneous fungal infections | clotrimazole |
| Concentrates in keratin (hair and nail beds) | terbinafine |
| SE: headache, GI, taste disturbances, symptomatic hepatobiliary dysfunction (cholestatic hepatitis) | terbinafine |
| Not recommended for patients on cyclosporine due to elevated alanine transaminase levels | caspofungin |
| Indications for caspofungin | invasive Aspergillus (when itraconazole and Amp B fail) and invasive Candida species |
| MOA of Griseofulvin | inhibits the mitotic spindle of dividing fungal cells by interacting with microtubules (fungistatic) |
| Indicated for the treatment of dermatophytes | Griseofulvin |
| Accelerates the hepatic metabolism of coumadin, estrogens and oral contraceptives | Griseofulvin |
| First line therapy for M. tuberculosis | RIPE, streptomycin |
| First line therapy for M. avium complex | clarithromycin, ethambutol, clofazimine, ciprofloxacin, amikacin |
| MOA: interferes with mycolic acid synthesis, disrupting cell wall synthesis | isoniazid |
| Administration routes of isoniazid | oral, IM |
| Correction of peripheral neuropathy with isoniazid | vitamin B6 supplementation |
| Interacts with Al+++ containing products that decreases absorption | isoniazid & ethambutol |
| Corticosteroids decrease efficacy | isoniazid |
| inhibits the CYP450 isozyme responsible for metabolizing phenytoin | isoniazid |
| MOA: binds to beta subunit of RNA pol and inhibits RNA synthesis | rifampin |
| Discolors body fluids to orange-red | rifampin |
| Serum levels increased by probenecid, competing for renal excretion | rifampin |
| Indications for rifampin | first line against TB, also used in MRSA and MRSE (with vancomycin and/or gentamycin), prophylaxis of meningitis, eradication of staph in nasal carries, antileprosy agent |
| Half-life of 3.5 hours - extends to 15 hours with renal disease | ethambutol |
| SE: optic neuritis, allergic reactions, hyperuricemia | ethambutol |
| MOA: converstion to active metabolite decreases the local pH below the threshold for growth | pyrazinamide |
| Active against tubercle bacilli in the acidic environment of lysosome and macrophage | pyrazinamide |
| SE: hepatotoxicity, non-gouty arthritis, hyperuricemia | pyrazinamide |
| MOA: inhibits cell wall synthesis by blocking L-alanine racemase and D-alanine synthetase | cycloserine |
| Indications for cycloserine | pulmonary and extrapulmonary TB, but only in pretreatment and when others fail |
| Contraindications for cycloserine | persons with history of epilepsy |
| SE: CNS, psyschotic states with suicidal tendencies, paranoia, seizures | cycloserine |
| Administered IM, nephrotoxic, last line TB agent (in combination) and multi-drug resistant therapy | capreomycin |
| Reserved as last line agent because of GI, hepatic, thyroid toxicity | ethionamide |
| Disease characterized by weight loss, fever, coughing | TB |
| Disease characterized by paroxysmal chills and fever | malaria |
| Resistance by P-glycoprotein, a protein efflux pump through the membrane | chloroquine |
| Loading dose required, binds strongly to cells containing melanin | chloroquine |
| Half-life is 6-7 days, but may be detectable for months or years | chloroquine |
| SE: visual impairment, ototoxicity, myopathy, peripheral neuropathy | chloroquine |
| Most versatile against Plasmodium, especially P. falciparum | chloroquine |
| Indicated for the treatment of extraintestinal amebiasis | chloroquine |
| Used when metronidazole is contraindicated | chloroquine |
| Combine with paramomycin for intestinal colonization | chloroquine |
| MOA of quinine | binds to DNA and inhibits nucleic acid biosynthesis |
| Not used for prophylaxis, more toxic and less effective than chloroquine | quinine |
| Worst therapeutic index of the anti-malarial agents | quinine |
| SE: cinchonism, depressive effects of the myocardium and dilation of vascular smooth muscle, QT prolongation, contraction of uterine smooth muscle | quinine |
| Prototype blood schizonticide for chloroquine and multi-drug resistant falciparum, often combined with doxycycline or clindamycin | quinine |
| T or F: quinine contraindicated in pregnancy | True |
| Indications for quinine gluconate | gametocidal to P. vivax and P. malariae, not falciuparum, more active than quinine to falciparum, life-threatening P. falciparum and antiarrhythmic agent |
| Malarial drug that has increased excretion with acidification of the urine | quinidine gluconate |
| SE: anticholinergic effects, avoid in pts. with AV block due to interference with HTN therapy | quinidine gluconate |
| Malarial drug that concentrates in the RBCs | mefloquine |
| SE: visual disturbances, insomnia, nightmares | mefloquine |
| Contraindicated with history of seizures, severe neuropsychiatric disturbances or adverse reactions to quinolone antimalarials | mefloquine |
| Indications for mefloquine | first line prophylaxis in chloriquine-resistant areas, alternative to quinine for acute falciparum, not for pregnant women (wait 3 months) |
| Indicated for asexual erythrocytic stages and not useful for laten tissue forms of P. vivax or gametocytes | halofantrine |
| Administer dose two hours before or after meals | halofantrine |
| SE: prolong QT interval, ventricular arrhythmias, fatty foods can exacerbate toxicity bt increasing absorption | halofantrine |
| Halofantrine indications | alternative to quinine and mefloquine for acute attacks of chloroquine or MDR stains of P. falciparum |
| MOA: converted in vivo to dihydrotriazine, which inhibits the bifunctional DHFR-thymidylate enzyme | chloroguanide |
| Indications for chloroguanide | Prophylactic treatment (combined with chloroquine) of falciparum malaria or mixed vivax and falciparum |
| Active drug against the late hepatic stages and latent tissue forms of P. vivax and P. ovale - a radical cure for relapsing malarias | primaquine |
| Indications for primaquine | Terminal prophylaxis and radical cure of P. vivax and ovale, but not falciparum (combined with blood schizontocide for increased effect) |
| Alternative treatment for mild to moderate PC pneumonia with clindamycin | primaquine |
| SE: hemolytic anemia, dark urine, anorexia, pallor, tiredness | primaquine |
| MOA: inhibits DHFR; schizonticidal for P. falciparum but not vivax | pyrimethamine |
| Should be used in combination with sulfadoxine | pyrimethamine |
| SE: skin rash, depression of hematopoeisis, megaloblastic anemia | pyrimethamine |
| Indications for pyrimethamine | Chloroquine-resistant falciparum in combination with sulfadoxine and quinine and the treatment of taxoplasmosis with sulfonamide or clindamycin |
| T or F: pyrimethamine can be used as a single agent | False |
| Administration routes of artemisinins | oral, IM, IV, rectal |
| With repeated dosing, can induce own P450-mediated metabolism | artemisinins |
| Indications for artemisinins | initial treatment for severe P. falciparum |
| Indications for metronidazole | first line drug for Ameobae, Giardia, Trichomonas |
| Administration routes of metronidazole | oral, IV, topically |
| SE: neurological toxicity, lithium toxicity, disulfiram effect with alcohol | metronidazole |
| Anti-protozoan that interacts with coumadin and prolongs the prothrombin time | metronidazole |
| DOC for Entamoeba histolytica | metronidazole |
| DOC for Giardia lamblia | metronidazole |
| DOC for Bacteroides fragilis | metronidazole |
| DOC for C. dificile | metronidazole |
| MOA: selectively inhibits the mitochondrial electron transport system, inhibiting pyrimidine synthesis | atovaquone |
| Exerts a protozocidal effect on Pneumocystis | atovaquone |
| Alternative for Pneumocystis jiroveci pneumonia in AIDS patients, Taxoplasma gondii, Enameoba histolytica, Trichomonoas vaginalis, P. falciparum with malarone | atovaquone |
| Route of administration for pentamidine | inhalation, parenterally |
| SE: hypotension, hypoglycemia, blood dyscrasias, nephrotoxicity, cardiotoxicity | pentamidine |
| Indicated for Pneumocystis carinii pneumonia, prophylaxis, aslternate for visceral leishmaniasis and trypanosomiasis (African sleeping sickness) | pentamidine |
| SE: anemia, leucopenia, diarrhea, convulsions, thrombocytopenia, alopecia | eflornithine |
| Indicated for west African trypanosomiasis (T. brucei gambiense) | eflornithine |
| Indications for paromomycin | treatment of tapeworms, amebiasis, some anti-protozoal (visceral leishmaniasis) |
| DOC for cryptosporidiosis in AIDS patients (alone or with azithromycin) | paromomycin |
| Indicated for Giardiasis in pregnant women during first trimester | paromomycin |
| DOC for intesinal colonization with E. histolytica | paramomycin |
| Combined with metronidazole for amebic colitis and amebic liver abscess | paromomycin |
| MOA: inhibits the assembly of tubulin dimers into polymers, arresting microtubule formation | benzimidazoles |
| MOA: inhibits helminthe-specific fumarate reductase | thiabendazole |
| Benzimidazole with best oral absorption | thiabendazole |
| Topical formulation preferred in localized cutaneous larva migrans | thiabendazole |
| Teratogenic benzimidazoles | mebendazole, albendazole |
| SE: interference with the metabolism of xanthine derivatives, CNS symptoms, odoriferous urine | thiabendazole |
| DOC for nematodes including Ascarias (roundworm), Enterbius (pinworm), hookworm (Ancylostoma duodenale, Necator Americanus) | mebendazole, albendazole |
| MOA: binds to parasitic nicotinic receptors causing a depolarizing neuromuscular blockade, spastic paralysis of worm muscle, and release from the intestinal wall | pyrantel pamoate |
| DOC for Moniliformis infection | pyrantel pamoate |
| Alternative to mebendazole for intestinal nematodes | pyrantel pamoate |
| Ivermectin MOA: | increases the permeability of the membrane to Cl ions by inhibiting glutamate-gated Cl channels and GABA-gated channels, hyperpolarizing the nerve and muscle cells (paralysis) |
| Indicated for strongyloidiasis, onchocerca and other coexisting nematodes | ivermectin |
| Indicated for lymphatic filariasis | diethylcarbamazine |
| MOA: causes increased permeability to certain cations (Ca+) leading to increased muscular activity, contraction, spastic paralysis, etc | praziquantel |
| Contraindicated in patients with ocular schistosomiasis | praziquantel |
| DOC for liver, lung, intestinal flukes and adult cestodes (tapeworms) at low doses | praziquantel |
| MOA: inhibits respiration and glucose uptake by inhibiting the anaerobic generation of ATP during mitochondrial oxidative phosphorylation | niclosamide |
| SE: cysticerosis | niclosamide |
| Indications for niclosamide | used therapeutically as a second choice drug (to praziquantel) for tapeworm |
| T or F: isoflurane, desflurane and sevoflurane are all volatile | True |
| T or F: high lipid solubility = rapid action (inhalational anesthetics) | False, low lipid solubility = rapid action |
| T or F: desflurane and sevoflurane have more rapid onset than halothane but slower termination | False, more rapid onset and termination |
| T or F: isoflurane and desflurane are the least depressant inhalational anesthetics on cardiac output | True |
| T or F: nitrous oxide alone has severe CV effects | False, N2O has no significant effects on CV when used alone |
| T or F: nitrous oxide has good analgesia activity | True |
| Main SE of halothane | hepatic toxicity, arrhythmias |
| Main SE of enflurane | seizures, possible hepatic toxicity |
| Inhalational DOC | sevoflurane |
| SE of nitrous oxide | drowsiness, dizziness/vertigo, dysphoria, panic, amnesia, inappropriate laughing, paresthesias |
| SE: inappropriate laughing | nitrous oxide |
| Components of balanced anesthesia | relax muscles, relieve anxiety, prevent secretions, induce unconsciousness |
| T of F: benzodiazepines are more potent than barbiturates | False |
| IV anesthetic of choice for patients with a weak heart | etomidate |
| T or F: ketamine does not affect respiration rate | True |
| T or F: etomidate has significant effects on heart rate and cardiac output | False, etomidate does not affect HR or CO |
| IV anesthetic: polyphoria, enzyme induction (P450) | thiopental |
| IV anesthetic: short DOA, antiemetic, infusion syndrome | propofol |
| IV anesthetic: analgesic, IM route, intact pharyngeal or laryngeal reflexes, bronchodilator for refractory asthma, hallucations | ketamine |
| Hallucinations from ketamine are treated with | benzodiazepines |
| IV anesthetic: dissociated state, eyes open but unconscious and pain-free | ketamine |
| T or F: BZDs have minimal CV and respiratory depression when used alone | True |
| Opioids pros | absence of direct effects on heart, maintenance of regional bloodflow autoregulation, decreased airway reflexes, pain relieved but pt. arousable, no malignant hyperthermia |
| Opioids cons | incomplete amnesia, histamine-related reactions, increase blood requirements, prolonged respiratory depression, CV instability, nitrous oxide results in CV depression |
| CV effects of opioids | bradycardia, hypotension, hypertension |
| Major SE of opioids | dose-dependent respiratory depression, increased intracranial blood flow and pressure |
| Common SE of opioids | N/V, constipation, miosis |
| Indicated for opioid respiratory depression | naloxone, nalmefene |
| Droperidol | Used in neurolept analgesia, state of indifference, anti-emetic, anti-convulsant |
| Indications for neurolept-analgesia | radiology, endoscopy, burn dressing |
| Reminfentanil | very short acting opioid, potent analgesic activity, rapid onset and peak (1 min), short t1/2 (10-20 min), recovery rapid when administration is D/C (loss of analgesia) |
| DOC for long lasting analgesia | morphine |
| DOC for short lasting analgesia | fentanyl |
| Which is more lipid soluble, morphine or fentanyl? | fentanyl |
| Which opioid is more likely to cause N/V? morphine or fentanyl | morphine |
| Indications for chloral hydrate | conscious sedation for dental procedures and perioperatively for antianxiety/sedation |
| SE of chloral hydrate | vomiting or behavioral changes, respiratory depression, habit-forming (withdrawal leading to seizures, delerium and death if untreated) |
| T or F: succinylcholine can be used in children | False |
| MOA of malignant hyperthermia | intracellular calcium release from sarcoplasmic reticulum |
| Anesthetic of choice for asthmatic patient | ketamine |
| MOA of local anesthetics | block voltage-gated sodium channels, disrupting surface charge |
| Differential blockade of fibers | small diameter and/or non-myelinated fibers are blocked most easily |
| Local anesthetic with greatest bone penetration (denistry) | articaine |
| T or F: amide local anesthetics have a shorter DOA than the ester-type | False |
| Amide metabolism is affected by | CV status, liver disease, toxemia of pregnancy, cimetidine, volatile anesthetics, beta blockers |
| Ester metabolism is affected by | liver disease, pregnancy, chemotherapeutics, atypical enzyme activity |
| Minor toxicities required to stop injection of local anesthetic | ringing in ears, metallic taste, numbness of lips and tongue |
| Most common vasoconstrictors used with local anesthetics | epinephrine, levonordefrin |
| FDA approved to reverse the effects of local anesthesia by facilitating bloodflow to the anesthetized area | phentolamine |
| Epinephrine interaction possible with | beta blockers, TCAs, halothane, HTN, heart blcok, cerebral vascular insufficiency |
| Short acting local anesthetics | procaine, chloroprocaine |
| Intermediate acting local anesthetics | articaine, lidocaine, prilocaine, mepivacaine |
| Long acting local anesthetics | bupivacaine, ropivacaine, tetracaine |
| Anesthetics that produce methemoglobinemia | prilocaine, benzocaine |
| Antidote for methemoglobinemia | IV methylene blue (or ascorbic acid) |
| Bupivacaine | more potent and cardiotoxic than lidocaine/mepivacaine |
| Ropivacaine | reduced cardiotoxicity, greater safety margin |
| Always administered with articaine | epinephrine |
| Anesthetics in the mouth, pharynx, larynx, trachea, esophagus, urethra | benzocaine, dyclonine |
| Anesthetics on the skin, NOT muscous membranes | dibucaine, pramoxine |
| EMLA | eutectic mixture of local anesthetics (2 drugs) |
| TAC | topical anesthesia through cut skin (tetracaine, epinephrine, cocaine), ineffective on intact skin |
| How long is it recommended to avoid additional local anesthetics after tumescence? | 12-18 hours |
| Drugs used for central nerve block in regional anesthesia | epinephrine, clonidine |
| Systemis uses for local anesthetics | suppression of grand mal seizures, reduction of intracranial pressure, analgesia, cough suppression, cardiac dysrhythmias |
| Local anesthetics used IV for cardiac arrhythmias | lidocaine |
| Local anesthetics used orally for cardiac arrhythmias | tocainide, procainamide, flecainide |
| How long before should you give an oral drug for pre-anesthetic medication? | 60-90 min |
| How long before should you give a drug IM for pre-anesthetic medication? | > 20 min; preferably 30-60 min |
| Type of drugs given for sedation, amnesia, anxiolysis | benzodiazepines |
| T or F: BZDs provide analgesia | False |
| Drug that is anti-dopamine/cholinergic/histaminergic effects used to lower the seizure threshold in pre-anesthetics | promethazine (phenthiazine) |
| 1st generations AHs: bronchodilator, sedative, anxiolytic, analgesic for pre-anesthetics | hydroxyzine, diphenhydramine |
| T or F: cimetidine and ranitidine produce sedation | False |
| Opioids for pre-anesthetic | morphine, meperidine, codeine, hydrocodone |
| Problems with pre-anesthetic opioids | orthostatic hypotension, epigastric distress, anti-diarrheal, increased sphincter tone, N/V, increased GI secretions, respiratory depression, coma-inducing, mioisis-inducing |
| NSAIDs used post-op | ketorolac, ibuprofen |
| NSAIDs SE from post-op | post-surgical bleeding outside of GI tract, fracture healing |
| Methods to reduce aspiration pneumonitis | Neutralize stomach pH, reduce volume, H2RAs, anticholinergic agents |
| Antacids that neutralize gastric pH | alumnium or magnesium hydroxide, calcium or sodium carbonate, sodium and potassium citrate + citric acid |
| Gastrokinetic agent that accelerates gastric emptying | metoclopramide |
| 150 mL of water for gastric emptying | stomach senses fullness for natural gastric emptying |
| Anti-emetics used | serotonin receptor antagonists, dopamine antagonists, cholinergic antagonists |
| Serotonin receptor antagonists used as anti-emetic | ondansetron, granisetron, tropisetron |
| Dopamine antagonist used as anti-emetic | metoclopramide |
| Cholinergic antagonist used as anti-emetic | scopolamine |
| Anti-emetic used when patients have failed all other therapies | droperidol |
| Indicated for prophylaxis for allergic reaction for pre-surgery | cimetidine, diphenhydramine |
| Antimicrobial used to treat staph and strep | cefazolin |
| Antimicrobials preferred against bowel anaerobes | cefotetan and cefoxitin |
| Anticholinergics used pre-operatively to treat reflex bradycardia, block muscarinic effects of anticholinesterases and dry secretions | atropine, scopolamine, glycopyrrolate |
| Used for children under 10 years old for rapid sequence intubation | atropine |
| Used for increased intracranial pressure for rapid sequence intubation | lidocaine, fentanyl, vecuronium |
| Indicated for surgical hypotension | dopamine, phenylephrine, ephedrine |
| Indicated for surgical hypertension | nitroprusside (rapid acting vasodilator), trimethaphan (ganglionic blocker) |
| Used to reverse effects of some sedatives and inhalational agents | phystostigmine |
| Initial anaphylaxis management | stop drug, D/C anesthesia, give O2, give epinephrine, intravascular volume expansion |
| Fusion inhibitors | enfuvirtide, maraviroc |
| MOA: binds to gp41 of the viral envelope and prevents the conformational change that allows fusion of the viral and host cell membrane | enfuvirtide |
| SE: increased liklihood of bacterial pneumonia | enfuvirtide |
| MOA: chemokine receptor 5 antagonist, binds to CCR5 co-receptor | maraviroc |
| Substrate for both CYP3A4 and p-glycoprotein | maraviroc |
| Indications for maraviroc | treatment of CCR5-tropic HIV-1 |
| Maraviroc SE | possible liver and cardiac problems, bladder irritation, rash, musculoskeletal symptoms |
| Maraviroc DDI | CYP3A inducers or inhibitors (dosage adjustment needed with efavirenz and lopinavir/ritonavir) |
| MOA of NRTIs | competitive inhibitors of viral RT and chain terminators |
| NNRTI that reduces perinatal HIV transmission | nevirapine |
| NRTI metabolism | not by CYP450 enzyme system |
| NRTI metabolized into glucuronide | zidovudine |
| Alcohol affects metabolism of what NRTI | abacavir |
| SE: peripheral neuropathy, pancreatitis | didanosine, stavudine |
| SE: hypersensitivity reactions due to genetic predisposition | abacavir |
| Acid-labile NRTI that should be taken 30 min before or 2 hours after meals | didanosine |
| Zidovudine DDI | concurrent bone marrow suppressive drugs: ganciclovir, interferon-alpha, dapsone, 5-FC, vincristine, vinblastine |
| Didanosine/Stavudine DDI | ethambutol, isoniazid, vincristine, cisplatin augment neuropathy and pancreatitis |
| Didanosine DDI | ganciclovir increases plasma concentration 2x and methadone decreases concentration |
| Stavudine DDI | antagonizes zidovudine |
| Abacavir DDI | ethanol increases plasma concentration |
| Needs only two phosphorylation steps for activation (more rapid and complete conversion of drug to active metabolite) | tenofovir |
| Tenofovir SE: | increase in liver enzymes |
| NNRTIs | delavirdine, nevirapine, efavirenz |
| NNRTI indications | only HIV-1 infections |
| NNRTI MOA: | bind directly to hydrophobic pocket in RT inducing a conformational change in the active site and blocking enzyme activity (no phosphorylation) |
| NNRTI metabolism | by CYP450 enzymes |
| CYP3A4 inhibitor (increases PIs, rifabutin, clarithromycin) | delavirdine |
| CYP3A4 inducer (decreases PIs, rifabutin, clarithromycin, methadone, estradiol) | nevirapine, efavirenz |
| Nevirapine SE | elevated liver enzymes |
| Efavirenz SE | abnormal dreams, impaired concentration |
| Indicated for acute and chronic HIV-1 infected cells and monocytes and macrophages that are not affected by RT inhibitors | protease inhibitors |
| PI metabolism | by CYP450 enzymes |
| ________ increases the concentration of other PIs through CYP inhibition | ritonavir |
| PIs are potent inhibitors of ________ | CYP3A4 |
| Concurrent use of _________ leads to decrease of PIs | CYP450 inducers (rifampin) |
| Carbamazepine lowers the concentration of _______ | indinavir |
| __________ upregulates PIs | ketoconazole |
| __________ is augmented by PIs | sildenafil |
| _________ is reduced by ritonavir, lopinavir, tipranavir | methadone |
| __________ is reduced by PIs except indinavir | oral contraceptives |
| SE: GI distress, parasthesias, increased bleeding in hemophiliacs, hyperglycemia, insulin resistance, hyperlipidemia, fat wasting and redistribution, breast enlargement, osteoporosis | protease inhibitors |
| Ritonavir, tipranavir SE | hepatotoxicity |
| Indinavir SE | alopecia, kidney stones, renal insufficiency |
| Indications for acyclovir, valacyclovir | herpes simpex keratitis, latent HSV, fever blisters, genital herpes, VZV, HSV encephalitis, and CMB bone marrow transplant recipients |
| Acyclovir SE | renal insufficiency and CNS disturbances |
| Indicated for CMV retinitis in AIDS patients and against HSV | ganciclovir |
| SE: teratogenic, carcinogenic, mutagenic | ganciclovir |
| Indicated for oral alternative for acyclovir, effective against HBV following liver transplant | famciclovir |
| Not phosphorylated by viral TK | cidofovir |
| Indicated for acyclovir-resistant HSV and VZV | cidofovir |
| IV delays progression of CMV retinitis in HIV patients | cidofovir |
| Indicated for nucleoside-resistant HSV, VZV, CMV, CMV retinitis and HIV | foscarnet |
| Foscarnet SE | renal failure or dysfunction, N/V, anemia, fatigue |
| Anti-HSV agent resistance | mutated viral DNA pol, absense of HSV thymidine kinase or altered HSV-TK substrate specificity |
| Anti-HSV agent excretion | glomerular filtration, dose adjustment for dysfunction |
| Indications for amantadine and rimantadine | oral prophylaxis against influenze A and an alternative for vaccination in immunocompromised patients and the elderly |
| Amantadine SE | anorexia, nausea, CNS effects in elderly |
| Rimantadine SE | lower risk for CNS effects than amantadine |
| SE: orally inhaled causing nasal and throat discomfort | zanamir |
| Oseltamivir SE | N/V |
| MOA: natural viral inhibitors, potent cytokines possessing antiviral, immunomodulating and antiproliferative actions | interferons |
| Increase bioavailability when given with ibuprofen | adefovir |
| Combination of _______ & ________ showed additive anti-HBV activity | adefovir, lamivudine |
| Indicated for chronic HBV, HCV, HPV, HH-V8 (kaposi sarcoma) | interferons |
| SE: flu-like syndrome, myelosuppression, neurotoxicity, proteinuria | interferons |
| Food on ribavirin OB | increased with fatty meals, decreased with antacids |
| Azole that binds most in the CSF | fluconazole |
| Azole that is mostly protein bound | itraconazole |
| Azole most concentrated in the urine | fluconazole |
| TB drugs given IM | streptomycin, capreomycin |
| NRTI with longest t1/2 | lamivudine |
| Food with zidovudine OB | decreased with fatty meal |
| NNRTI with worst OB | efavirenz |
| NNRTI with shortest t1/2 | delavirdine |
| NNRTI least protein bound | nevirapine |
| Anti-HSV agent with best OB | famciclovir, penciclovir |
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