Pharm-2C

• 1. Prochlorperazine (Compazine)
• 2. Chlorpromazine (Thorazine)

most widely used antiemetics

AE: extrapyramidal effects, hypersensitivity, excessive sedation, anticholinergic effects, bone marrow suppression, skin reactions

(palonosetron)

-NEW injectable annit-vomiting and anti-nausea agent for chemotherapy

5-HT3 receptor antagonist

LONG half-life (40 hrs)

(Aprepitant)

-substance P/neurokinin 1 receptor antagonist for anti-vomitiing

-used in chemotherapy

-CYP 450 inhibitor

-oral and IV

(Phenergan)

antihistamine and anticholinergic agent used for simple N/V, motion sickness, vertigo

-IM and supp

(Tigan)

antihistamine and anticholinergic agent used for simple N/V, motion sickness, vertigo

-IM and supp

(Antivert or Bonine)

antihistamine and anticholinergic agent used for simple N/V, motion sickness, vertigo

(Dramamine)

antihistamine and anticholinergic agent used for simple N/V, motion sickness, vertigo

(Transderm Scop)

antihistamine and anticholinergic agent used for simple N/V, motion sickness, vertigo

-patch best for prevention of motion sickness

• 1. dry mouth
• 2. urinary retention
• 3. drowsiness
• 4. blurred visino
• 5. caution in BPH and narrow angle glaucoma

• 1. Droperidol (Inapsine)
• 2. Haloperidol (Haldol)

-used for complex cases of vomiting in anesthesia and chemo

-blocks stimulation of the CTZ

AE: sedation, dystonia, EP reactions which can be relieved by diphenhydramine

QT prolongation, ECG is recommended before treatment

increased risk of sudden cardiac death

(Reglan)

used for complex N/V and for gastroparesis associated with diabetic autonomic neuropathy

AE: EP effects, restlessness, drowsiness, diarrhea (may need to give with IV diphenhydramine)

• 1. Dexamethasone
• 2. Methylprednisolone (IV)

-for post-op and chemo induced

-increases appetite and feelings of well-being

AE: mood changes, HA, metallic taste, hyperglycemia and itchy throat

• 1. Ondasetron
• 2. Granisetron
• 3. Dolasetron

-block 5HT receptor for chemo N/V

AE: HA, diarrhea, dizziness, constipation

• 1. Dronabinol (Marinol)
• 2. Nabilone (Cesamet) - less euphoria

1. Combination of two or more agents

2. May combine metoclopramide, diphenhydramine and dexamethasone

3. Use a selective serotonin antagonist with dexamethasone for delayed effects

4. Benzodiazepines such as lorazepam are useful for anticipatory N/V

1. Common esp. with women, increased age and obesity

2. Selective serotonin antagonists are effective but expensive

3. Dexamethasone is effective as well

4. May use antihistamines in combination as well

-use antihistamines like deminhydrinate, meclizine, and promethazine

-associated with dopamine (metoclopramide, prochlorperazine)

anticholinergics and antihistamines

• -1st line is DA antagonist
• -2nd line is serotonin (5HT) antagonist

Prevention: 5HT antagonists, dexamethasone, droperidol

Treatment: DA antagonists, 5HT antagonists, drexamethasone

Antacid for heartburn

-neutralizes gastric acids

AE: aluminum causes constipation and magnesium can cause diarrhea

interferes with absorption of other drugs, Al salts may cause problems in renal insufficiency pts, cancium carbonate can form gas-bloating

1. Cimetidine (Tagamet) - most effect on cytochrome P450 --> drug interactions

2. Ranitidine (Zantac) - can be used w/ infants

3. Famotidine (Pepcid) - longest duration

4. Nizatidine (Axid)

-useful for mild to moderate GER

-not as effective as PPIs

• 1. Esomeprazole (Nexium)
• 2. Omeprazole (Prilosec)
• 3. Lansoprazole (Prevacid)
• 4. Rabeprazole (Aciphex)
• 5. Pantoprazole (Protonix)

PROLE

-P450 metabolism so drug interactions occur

-pregnancy cat B

agent of GERD

-sticky and viscous gel protects tissue

AE: constipation

1. H. pylori induced - duodenal

2. NSAID induced - gastric , deeper more GI bleeds

3. Stress ulcers - 10% of Americans develop it

Three drug: 2 abx (clarithromycin & metronidazole OR clarithromycin & amoxicillin) + PPI for 14 days

4 drug: 2 abx (tetracylcine & metronidazole) + bismuth + PPI

new 4 drug formulation to fight H.pylori

-Bismuth subcitrate potassium & metronidazole & tetracycline & omeprazole

PPIs are more effective in reducing gastric and duodenal ulcers (preferred choice)

H2 blockers should NOT be used as cotherapy with nonselective NSAID for prophylaxis

-cotherapy with misprostol and a prostaglandin analog for prevention of NSAID induced ulcers

synthetic prostaglandin analog that protect gastric mucosa; added w/ NSAID therapy to protect against ulcers

-Cat X!

MOA: prodrug which is activated to block mycolic acid synthesis, components of mycobacterial cell walls; Penetrates well into cells, CNS and infected tissue including granulomas

AE: hepatitis & peripheral neuropathy

monitor w/ LFTS; neuropathy avoided by pyridoxime

MAO: binds to beta subunit of bacterial DNA dependent RNA polmerase and inhibits RNA synthesis

AE: Harmless reddish orange discoloration of body fluids; may cause hepatitis, cholestasis w/ jaundice, and nephritis

Drug interactions -- induced P450, which increases elimination of oral contraceptives and protease inhibitors (HIV meds)

AE: hepatotoxicity, polyarthralgia (40%), N/V, hyperuricemia

AE: retrobulbar neuritis causing loss of color vision (green >> red) and loss of visual acuity

• 1. Isoniazid (INH)
• 2. Rifampin (RIF)
• 3. Pyrazinamide (PZA)
• 4. ethambutol

4 drug regiment + vitamin B6 for 2 month (initiation phase) followed by 18 week of INH and RIF (continuation phase)