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Pharmacology > Semester 2 > Flashcards

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
Q

What receptors are found in the vestibular system?

A

H1 receptors and ACh receptors

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26
Q

What receptors are found in the chemoreceptor trigger zone?

A

D2 receptors, 5HT3 receptors, and NK1 receptors

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27
Q

What receptors are found in the vomiting center?

A

ACh receptors, H1 receptors, 5HT2 receptors

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28
Q

What receptors are found in the GI tract?

A

D2 receptors and 5HT3 receptors

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29
Q

Prochlorperazine

A

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
Q

Metoclopramide

A

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
Q

Ondansetron

A

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
Q

Promethazine

A

Histamine H1 receptor antagonist - targets vestibular apparatus
Indications - motion sickness treatment and prevention
Adverse effects - sedation

33
Q

Scopolamine

A

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
Q

Corticosteroids used to treat nausea/vomiting

A

Prednisone and Dexamethasone

Treat nausea due to increased intracranial pressure

35
Q

Benzodiazapenes used to treat nausea/vomiting

A

Lorazepam and Diazepam

Treat anxiety-associated nausea and vomiting

36
Q

Causes and findings seen in cholinergic/anticholinesterase syndrome

A

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
Q

Causes and findings seen in anticholinergic syndrome

A

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
Q

Causes and findings seen in hemoglobinopathy syndromes

A

Carboxyhemoglobinemia - due to CO poisoning
Methemoglobinemia - sulfonamides
Symptoms - hypoxia; headache; disorientation; coma; nausea; vomiting; acidosis; death

39
Q

Narcotic overdose

A

Caused by heroine, oxycodone, morphine, and meperidine

Symptoms - pinpoint pupils; respiratory depression and hypotension

40
Q

Sympathomimetic excess

A

Caused by cocaine, amphetamines, MAOIs

Symptoms - nervousness, agitation, tremor, diaphoresis, CNS excitation, hypertension, tachycardia

41
Q

What are the symptoms of opiate withdrawal?

A

Mydriasis (dilated pupils), piloerection, rhinorrhea, lacrimation

42
Q

What are the symptoms of CNS depressant withdrawal?

A

Hallucinations, tachycardia, hyperpyrexia (high fever), seizures

43
Q

Which drug can cause AV blockade?

A

Digitalis

44
Q

Which drugs can lead to sinus bradycardia?

A

Digitalis, beta blockers, CCBs

45
Q

Which drugs can lead to sinus tachycardia?

A

Cocaine and amphetamines (plus many types of poisonings and non-toxicological conditions)

46
Q

What are some causes of metabolic acidosis?

A

ASA, methanol, ethylene glycol, DKA, lactic acidosis (think MUDPILES and HARD ASS)

47
Q

How do you go about treating seizures (both acutely and long term)?

A

Acute control - diazepam/lorazepam

Long term management - phenobarbital

48
Q

What are 4 methods for removing toxic agents from the gut?

A

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
Q

Modalities for eliminating absorbed substances

A 
Repeated doses of charcoal
Forced diuresis
Ion trapping in urine
Hemodialysis
Hemoperfusion
50
Q

Chloroquine

A

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
Q

Mefloquine

A

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
Q

Atovaquone

A

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
Q

Doxycycline

A

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
Q

Quinine/Quinidine

A

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
Q

Primaquine

A

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
Q

Artemisinin

A

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
Q

Metronidazole

A

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
Q

Iodoquinol

A

Treats luminal amoebic infections

Adverse effects - neurotoxicity and nausea and vomiting

59
Q

What agents are used to treat Giardia?

A

Metronidazole, nitazoxanide

60
Q

Cryptosporidiosis

A

General - lactose free diet, antimotility agents, restoration of immune response in HIV patients (HAART therapy)

61
Q

What is the drug of choice for treating cryptosporidiosis?

A

Nitazoxanide

62
Q

What agents are used to treat toxoplasmosis?

A

Pyrimethamine - need to add folinic acid + sulfadiazine/clindamycin (no role for montherapy)

63
Q

What agents are used to treat Leishmaniasis?

A

Sodium stibogluconate - mainstay for cutaneous and visceral leishmaniasis
Adverse effects - Fever, myalgias, arthralgias, QT prolongation
Others: Amphotericin B (normal and liposomal), Miltefosine

64
Q

What agents are used to treat African Trypanosomiasis?

A

Suramin - hemolymphatic disease
Pentamidine - does not cross BBB
Melarsoprol
Eflonithine

65
Q

What agents are used to treat American Trypanosomiasis?

A

Nifurtimox and Benznidazole

66
Q

Nifurtimox

A

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
Q

Neurocysticercosis treatment

A

Controversial - albendazole and praziquantel

Albendazole more efficacious, has less interactions than corticosteroids and anticonvulsants

68
Q

Albendazole

A

Useful in pinworms, ascariasis, hookworm, trichuriasis, strongyloides, echinococcus, neurocysticercosis

69
Q

Praziquantel

A

Schistosoma, chlonorchiasis, paragnomiasis
ADRs - headache, drowsiness, dizziness, abdominal pain
Contraindications - ocular cysticercosis
Precautions - pregnancy and lactation

70
Q

Mebendazole

A

Interactions - carbamazepine, dilantin

71
Q

Pyrantel pamoate

A

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
Q

Ivermectin

A

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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