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Semester 2 Flashcards

1
Q

What is a noteworthy adverse effect of antacid use?

A

Milk-alkali syndrome: hypercalcemia, alkalosis, renal impairment

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2
Q

Name 4 histamine antagonists

A

Ranitidine
Famotidine
Cimetidine
Nizatidine

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3
Q

H2 antagonist MOA

A

Inhibit acid secretion, preventing NSAID-induced ulcers and healing peptic ulcers

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4
Q

What type of drug should not be given with an H2 antagonist and why?

A

Antacids - reduce H2 antagonist serum concentration to 1-20%

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5
Q

PPI MOA

A

Irreversibly bind to and inhibit H/K ATPase pump on luminal surface of parietal cell membrane
Block parietal cell acid secretion

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6
Q

What are the 3 phases of activation of PPIs?

A

1 - weak bases concentrated in acid compartment of parietal cell
2 - prodrug converted to active form in acidic environment
3 - sulfhydryl group forms disulfide bond with cysteine residue on H/K ATPase - inactivates the enzyme

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7
Q

When should PPIs be taken to optimize activity?

A

30-60 minutes before a meal - ensures PPI is in bloodsteam in post-prandial hours when parietal cells stimulated

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8
Q

Name 5 PPIs

A 
Omeprazole
Lansoprazole
Rabeprazole
Pantoprazole
Esomeprazole
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9
Q

PPIs shouldnt be given with ___ because they reduce the efficacy of PPIs

A

H2 antagonists

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10
Q

PPIs are the drug of choice for treating which conditions?

A

Zollinger-Ellison syndrome and GERD when not responsive to H2 antagonists

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11
Q

PPI Drug Interactions

A

PPIs metabolized by CYP 450 - decrease clearance of benzodiazopines, warfarin, and phenytoin
Reduce absorption of ketoconazole
Increase absorption of digoxin
Prolonged use can lead to B12 deficiency (need acidic parietal cell environment for B12 absorption)

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12
Q

Pepto-Bismol MOA

A

Acts like sucralfate - adheres to necrotic tissue and creates a barrier between gastric contents and the mucosa
Useful for treating duodenal ulcers and suppression of H. pylori

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13
Q

H. pylori treatment guidelines

A

Triple therapy - PPI + 2 ABXs - 1 week course of treatment has a 90% cure rate
If only 1 ABX used, therapy must last 2 weeks and cure rate is 10-29% lower

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14
Q

Bulk Laxative

A

Examples - dietary fiber, psyllium
MOA - increase stool weight, retention of fluid in stool, stimulate peristalsis
Adverse effects - flatulence
requires increased fluid intake - do not use in debilitated patients who cannot drink adequate fluid - may lead to worsened constipation

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15
Q

What are two nonabsorbable sugar laxatives?

A

Lactulose and Sorbitol - used for constipation
MOA - bacteria degrade sugars in colon, increase osmotic pressure and stool water content
Side effects - bloating, cramps, “sickly sweet”
Indications - constipation

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16
Q

What are the saline and magnesium salts?

A 
Magnesium citrate
Magnesium hydroxide (milk of magnesia)
Sodium phosphate (Fleets Phospho-Soda)
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17
Q

Saline and magnesium salt laxatives - MOA

A

Pull water into stool and help propel food forward to stimulate peristalsis
Mg stimulates CCK
Side effects/contraindications - bowel obstruction; dehydration; electrolyte abnormalities; ischemic colitis
Important - do not use in patients with RF (may develop hypermagnesemia and phosphatemia) or CHF (fluid overload)

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18
Q

What is an important side effect of sodium phosphate laxatives?

A

Acute phosphate nephropathy - deposition of calcium in tubules leading to obstruction
Risk factors - old age, CHF, hepatic/renal insufficiency

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19
Q

What are saline and magnesium salt laxatives used to treat?

A

Mag citrate + sodium phosphate - bowel prep

Mag hydroxide - constipation (more gentle, fewer side effects)

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20
Q

What are the four noteworthy polyethylene glycol laxatives and their indications?

A

Miralax and Glycolax - used for constipation

Colyte, Golytely - bowel prep

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21
Q

MOA and indications of polyethylene glycol laxatives

A

MOA - osmotically active, stays in bowel and retains water in the stool
Indications - constipation (at small doses), bowel prep (at high doses)

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22
Q

What are two important stimulant laxatives?

A

Senna and Bisacodyl (Dulcolax)
Senna - converts to active metabolic in colon, stimulates myenteric plexus
Bisacodyl - stimulates sensory nerve endings, parasympathetic stimulation
Side effects - cramping, melanosis coli
Indications - constipation (particularly opiate induced)

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23
Q

Detergent laxatives (stool softeners)

A

Docusate (colase)
MOA - increases penetration of water into stool - acts like a surfactant and allows mixing of water with stool
Indications - prevents formation of hard stool

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24
Q

Lubricants

A

Glycerin suppository/enema - lubricates stool and stimulates rectal contractions (irritant)
Mineral oil enema - softens stool, may be ingested but do not give orally to sick, debilitated patients - can get lipid pneumonitis
Indications - fecal impaction

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25
What receptors are found in the vestibular system?
H1 receptors and ACh receptors
26
What receptors are found in the chemoreceptor trigger zone?
D2 receptors, 5HT3 receptors, and NK1 receptors
27
What receptors are found in the vomiting center?
ACh receptors, H1 receptors, 5HT2 receptors
28
What receptors are found in the GI tract?
D2 receptors and 5HT3 receptors
29
Prochlorperazine
Dopamine receptor antagonist Centrally - blocks chemoreceptor trigger zone Peripherally - blocks vomiting stimuli carried by Vagus nerve Indications - opioid related nausea/vomiting; GI disorders, inflammation, infection Adverse Effects - Extrapyramidal effects (blocking dopamine receptors); dystonia
30
Metoclopramide
Dopamine receptor antagonist MOA - blocks D2 receptor in chemoreceptor trigger zone Indications - chemo induced nausea/vomiting; treatment of UGI tract dysmotility (diabetic gastroparesis, gastric stasis) Adverse Effects - Extrapyramidal effects (tardive dyskinesia); dystonia (trismus, torticollis - treated with anticholinergics)
31
Ondansetron
5HT3 antagonist - works centrally and peripherally Indications - chemo and radiation induced nausea/vomiting and prophylaxis; post op nausea/vomiting Adverse Effects - QT prolongation (may lead to Torsades de Pointes); headache
32
Promethazine
Histamine H1 receptor antagonist - targets vestibular apparatus Indications - motion sickness treatment and prevention Adverse effects - sedation
33
Scopolamine
Pure anticholinergic - works in vestibular apparatus Indications - motion sickness Adverse effects - confusion; urinary retention; acute narrow angle glaucoma; dry mouth (all due to parasympathetic blockade)
34
Corticosteroids used to treat nausea/vomiting
Prednisone and Dexamethasone | Treat nausea due to increased intracranial pressure
35
Benzodiazapenes used to treat nausea/vomiting
Lorazepam and Diazepam | Treat anxiety-associated nausea and vomiting
36
Causes and findings seen in cholinergic/anticholinesterase syndrome
Causes - organophosphate and carbamate insecticides Symptoms due to large concentrations of ACh stimulating nicotinic/muscarinic receptors Muscarinic symptoms - miosis; lacrimation; sialorrhea; wheezing; vomiting; bradycardia; hypotension Nicotinic symptoms - anxiety; restlessness; seizure; coma
37
Causes and findings seen in anticholinergic syndrome
Causes - atropine, scopolamine, tricyclic antidepressants, antihistamines, jimson weed Peripheral effects (blockade of muscarinic receptors - dry mouth; dysphagia; blurred vision; mydriasis; tachycardia; hyperthermia; flushing; abdominal distention Central effects - lethargy; excitement; seizure; confusion; hallcuination; coma; ataxia; respiratory failure
38
Causes and findings seen in hemoglobinopathy syndromes
Carboxyhemoglobinemia - due to CO poisoning Methemoglobinemia - sulfonamides Symptoms - hypoxia; headache; disorientation; coma; nausea; vomiting; acidosis; death
39
Narcotic overdose
Caused by heroine, oxycodone, morphine, and meperidine | Symptoms - pinpoint pupils; respiratory depression and hypotension
40
Sympathomimetic excess
Caused by cocaine, amphetamines, MAOIs | Symptoms - nervousness, agitation, tremor, diaphoresis, CNS excitation, hypertension, tachycardia
41
What are the symptoms of opiate withdrawal?
Mydriasis (dilated pupils), piloerection, rhinorrhea, lacrimation
42
What are the symptoms of CNS depressant withdrawal?
Hallucinations, tachycardia, hyperpyrexia (high fever), seizures
43
Which drug can cause AV blockade?
Digitalis
44
Which drugs can lead to sinus bradycardia?
Digitalis, beta blockers, CCBs
45
Which drugs can lead to sinus tachycardia?
Cocaine and amphetamines (plus many types of poisonings and non-toxicological conditions)
46
What are some causes of metabolic acidosis?
ASA, methanol, ethylene glycol, DKA, lactic acidosis (think MUDPILES and HARD ASS)
47
How do you go about treating seizures (both acutely and long term)?
Acute control - diazepam/lorazepam | Long term management - phenobarbital
48
What are 4 methods for removing toxic agents from the gut?
Syrup of ipecac - best when given at home Gastric lavage - depends on size of particle, patient age Activated charcoal - adsorbable material (may be constipating so given with sorbitol/saline cathartic agent) Whole bowel irrigation - Golytely or sustained release preparation
49
Modalities for eliminating absorbed substances
``` Repeated doses of charcoal Forced diuresis Ion trapping in urine Hemodialysis Hemoperfusion ```
50
Chloroquine
Used for prophylaxis and treatment Schizonticidal in blood to all plasmodium species but not activate against liver phase parasites (vivax and ovale) MOA - prevents polymerization of heme to hemozoin Adverse Effects - pruritis **Resistance to chloroquine is widespread, especially in falciparum**
51
Mefloquine
Prophylaxis in areas of chloroquine-resistant falciparum Adverse Effects - nausea, vomiting, neuropsychiatric toxicities (seizure, psychosis) Contraindications - seizures, psych disturbances, arrhythmia Interactions - Quinine, Quinidine, Halofantrine
52
Atovaquone
MOA - inhibits parasite mitochondrial electron transport Given with proguanil as Malarone (less resistance) Has to be given daily Better tolerated than mefloquine for prophylaxis
53
Doxycycline
MOA - protein synthesis inhibitor Indications - prophylaxis against mefloquine-resistant plasmodium falciparium Has to be given daily Not recommended for prophylaxis in children or pregnant women
54
Quinine/Quinidine
Drug of choice for treating severe disease with chloroquine resistant P. falciparum malaria Quinine = oral; Quinidine = IV Can be used with doxycycline to shorten duration and limit toxicity Adverse effects - Cinchonism - headache, nausea, visual disturbance Quinine can be used if needed in pregnancy
55
Primaquine
Used to treat exoerythrocytic forms of vivax and ovale Drug of choice for radical cure after chloroquine Adverse effects - nausea, abdominal pain, cramps Contraindications - may lead to hemolytic anemia in individuals with G6PD deficiency
56
Artemisinin
Rapidly acting schizonticide - second agent used to prevent MOA - production of toxic free radicals in parasite food vacuole IV artesunate - available for treatment of severe malaria in the US Coartem (artemether/lumenfantrine) - treatment of uncomplicated falciparum malaria
57
Metronidazole
Drug of choice for extraluminal amebiasis (used for dysentery, ameboma, liver abscess) MOA - ferredoxin-linked processes reduce nitro group to a product that is lethal against anaerobic organisms Adverse Effects - nausea, vomiting, metallic taste, disulfuram-like
58
Iodoquinol
Treats luminal amoebic infections | Adverse effects - neurotoxicity and nausea and vomiting
59
What agents are used to treat Giardia?
Metronidazole, nitazoxanide
60
Cryptosporidiosis
General - lactose free diet, antimotility agents, restoration of immune response in HIV patients (HAART therapy)
61
What is the drug of choice for treating cryptosporidiosis?
Nitazoxanide
62
What agents are used to treat toxoplasmosis?
Pyrimethamine - need to add folinic acid + sulfadiazine/clindamycin (no role for montherapy)
63
What agents are used to treat Leishmaniasis?
Sodium stibogluconate - mainstay for cutaneous and visceral leishmaniasis Adverse effects - Fever, myalgias, arthralgias, QT prolongation Others: Amphotericin B (normal and liposomal), Miltefosine
64
What agents are used to treat African Trypanosomiasis?
Suramin - hemolymphatic disease Pentamidine - does not cross BBB Melarsoprol Eflonithine
65
What agents are used to treat American Trypanosomiasis?
Nifurtimox and Benznidazole
66
Nifurtimox
Drug of choice for active T. cruzi Decreases severity of infection and eliminates detectable parasites - does not eradicate infection and not effective against chronic disease Adverse Effects - GI, rash, CNS
67
Neurocysticercosis treatment
Controversial - albendazole and praziquantel | Albendazole more efficacious, has less interactions than corticosteroids and anticonvulsants
68
Albendazole
Useful in pinworms, ascariasis, hookworm, trichuriasis, strongyloides, echinococcus, neurocysticercosis
69
Praziquantel
Schistosoma, chlonorchiasis, paragnomiasis ADRs - headache, drowsiness, dizziness, abdominal pain Contraindications - ocular cysticercosis Precautions - pregnancy and lactation
70
Mebendazole
Interactions - carbamazepine, dilantin
71
Pyrantel pamoate
Useful for pinworm, ascaris, hookworm Luminal agent - depolarizing neuromuscular blocking agent (release of ACH/inhibition of ACHase resulting in worm paralysis) Precautions - liver diseases, kids under 2 and pregnancy
72
Ivermectin
Treatment of choice for strongyloides and onchocerciasis (river blindness) MOA - paralyzes nematodes by intensifying GABA-mediated signals Adverse Effects - Mazotti reaction - fever, headache, dizziness (seen in severe onchocerciasis)

Pharmacology (5 decks)

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