Pharma - Evals 6 Flashcards
Best time to administer a PPI
30-60 minutes before meal
Triple therapy for H. pylori
Omeprazole 20 mgBID
Clarithromycin 500mg BID
Amoxicillin 1g (or Metronidazole 500mg) BID
14 days
Quadruple therapy for H. pylori
Omeprazole 20 mgBID Metronidaxole 500mg TID Bismuth subsalicylate 525mg QID Tetracycline 500mg QID 14 days
Enzymes that primarily metabolize PPIs
CYP3A4
CYP2C19
Cytoprotective actions of Misoprostol ay 20mcg
Increase mucus and bicarbonate production
Enhance mucosal blood flow
Maintains tight junction between epithelial cells
Anti-H. pylori antibacterials
Clue: MCBAT
Metronidazole Clarithromycin Bismuth subsalicylate Amoxicillin Tetracycline
Cytoprotective drugs
Prostaglandin analogs (Misoprostol)
Sucralfate
Bismuth Chelate
AE of Misoprostol
Uterine contraction leading to abortion
Diarrhea
Abdominal cramps
AE of Ranitidine
Headache, drowsiness
Diarrhea
Rashes
Arrhythmia (with rapid IV infusion)
AE of Sucralfate
Constipation (most common)
Dry mouth, nausea, vomiting
Aluminum overload in px with renal dysfunction
Benzoar development
Activation site of Omeprazole
Parietal cells cannaliculi
MOA of Benzimidazoles (Albendazole and Mebendazoles)
Inhibits microtubule polymerization by binding to beta-tubulin
MOA of Ivermectin
Binds to glutamate-activated Cl- channels in nematode muscles causing hyperpolarization and TONIC PARALYSIS
Intensifies GABA-mediated neurotransmission in nematodes
Albendazole intake for tissue parasites
After a fatty meal
Albendazole intake for luminal parasites
Empty stomach
DOC for filariasis, loaisis and tropical eosinophilia
Diethylcarbamazine
DOC for cestodes and temodes + all Schistosoma
Praziquantel
DOC for pinworm (can be used for hookworm/A. duodenale or N. americanus)
Pyrantel pamoate
DOC for strongyloides (threadworm) and onchocerciasis
Ivermectin
MOA of praziquantel
Calcium ion influx causing contraction of schistosome muscles resulting in appearance of small holes and balloon-like structures which will make the parasite vulnerable to antibody binding and leukocyte killing;
SPASTIC PARALYSIS
DOC for hydatid disease and ascariasis (roundworm) + cysticercosis (T. solium)
Albendazole
Ovicidal and Larvicidal
DOC for whipworm (Trichuris)
Mebendazole
Ovicidal - Ascaris and Trichuris EGGs
Larvicidal - larva and adult stage of nematodes
MOA of Diethylcarbamazine
Piperazine derivative that causes direct effect to microfilariae of W. bancrofti which leads to organelle damage and eventually apoptosis
MOA Praziquantel
Increases the permeability of trematode and cestode cell membranes to calcium, causing paralysis, dislodgement and death
MOA of Pyrantel Pamoate
Persistent activation of nicotinic cholinergic receptor resulting in SPASTIC PARALYSIS of the worm
Mazzoti reaction
Exacerbationof the immune system due to dying bodies of the parasites
Produces fever, headache, dizziness, rashes, tachycardia, hypotension and arthralgia
Drugs that cause Mazzoti reaction
Ivermectin and Diethylcarbamazine
Pregnancy considerations of Benzimidazoles
Beneficial for 2nd and 3rd trimester
Avoided during 1st
Major excretory pathway of tissue amoebicides
Urine
DOC for intestinal amoebiasis (oral)
Paromomycin sulfate
DOC for extraluminal amoebasis (amebic colitis and amebic liver disease), giardiasis, trichomaniasis
(Kills trophozoites, not cysts of E. histolytica)
Metronidazole
MOA of Metronidazole
Reactive reduction of nitro group
Effect of Metronidazole on alcohol
Stop acetaldehyde dehydrogenase causing accumulation of acetaldehyde, leading to hypotension
DOC for severe intestinal and extraintestinal amoebiasis if metronizadole is CI
Dehydroemetine
DOC for non-falciparum malaria + amebic liver abscesses only
Clue: Also a DMARD
Chloroquine
Luminal amoebicide that is CI in px with thyroid ds
Alternative for intestinal amoebiasis
Iodoquinol
Alternative drug for amoebiasis during 1st trimester
Paromomycin sulfate
AE of tetracycline
Tooth discoloration
Bone development in fetus
Drug-induced lupus
DOC for asymptomatic luminal infection (as a single agent)
Diloxanide furoate
MOA of Nitazoxanide
Converted to TIZOXANIDE (active metab) to inhibi PFOR dependent enzymes but does not produce DNA mutations
Pregnancy considerations for Metronidazole
Crosses the placenta
Theoretical risk to fetus, not recommended in early pregnancy
Two metabolites of Diloxanide furoate
Diloxanide
Furoic acid
Uses of Nitazoxanide
E. histolytica Giardia T. vaginalis C. parvum H. nana T. trichiura H. pylori (pediatric) A. lumbricoides F. hepatics Several tapeworms Metronidazole-resistant protozoal strains
MOA of Neostigmine
Amplifies action of Ach, increasing parasympathetic activity and somatic neuromuscular transmission
Action of Metoclopramide
D2 receptor antagonism
5-HT4 agonism
Vagal and Central 5-HT3 antagonism
Possible sensitisation of muscarinic receptors on smooth muscles (most effective for GERD)
AE of Metoclopramide
Extrapyramidal effects
Galactorrhea
Methemoglobinemia in premature and full term infants
Prokinetic that has most potential to induce serious and fatal arrhythmias when combines with other drugs that inhibit CYP3A4
Cisapride
Anti-secretory agent best used for the treatment of “dumping syndrome” after gastric surgery or pyroplasty
Octreotide
Hexose nucleus of Streptomycin
Streptidine
Hexose nucleus for all other aminoglycosides
2-deoxystreptamine