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nizatidine (Axid)

 

Classes: Histamine H2 Antagonists

Dosing and uses of Axid (nizatidine)

 

Adult dosage forms and strengths

capsule

  • 150mg
  • 300mg

oral solution

  • 15mg/mL

tablet

  • 75mg

 

Active Duodenal Ulcer

300 mg PO qHS Or

150 mg PO q12hr

Most heal after 4 weeks

 

Duodenal Ulcer Maintenance

150 mg PO qHs

 

Benign Gastric Ulcer

300 mg PO qHS Or

150 mg PO q12hr

 

GERD

150 mg PO q12hr Or

300 mg PO qHs

 

Renal Impairment

Active duodenal ulcer, gastric ulcer, GERd

  • CrCl 20-50 mL/min: 150 mg PO qDay
  • CrCl <20 mL/min: 150 mg PO qOTHERday

Duodenal ulcer maintenance

  • CrCl 20-50 mL/min: 150 mg PO qOTHERday
  • CrCl < 20 mL/min: 150 mg PO q3Days

 

Other Indications & Uses

Heartburn (OTC product)

 

Pediatric dosage forms and strengths

capsule

  • 150mg
  • 300mg

oral solution

  • 15mg/mL

tablet

  • 75mg

 

GERD

<12 years: 5-10 mg/kg/day PO divided q12hr (limited data)

 

Geriatric dosage forms and strengths

 

Active duodenal ulcer

300 mg PO qHS Or

150 mg PO q12hr

Most heal after 4 weeks

 

Duodenal ulcer maintenance

150 mg PO qHs

 

Benign gastric ulcer

300 mg PO qHS OR150 mg PO q12hr

 

GERD

150 mg PO q12hr Or

300 mg PO qHs

 

Axid (nizatidine) adverse (side) effects

>10%

Headache (17%)

 

1-10%

Abdominal pain

Anxiety

Constipation

Diarrhea

Dizziness

Insomnia

Nausea/vomiting

Pruritus

 

<1%

Anemia

Increased LFT's

 

Warnings

Contraindications

Hypersensitivity to nizatidine or other H2 receptor antagonists

 

Cautions

Adjust dosage in renal impairment

May see false positive urobilinogen secondary to nizatidine

 

Pregnancy and lactation

Pregnancy category: C

Lactation: crosses into breast milk, either discontinue nursing or the drug

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Axid (nizatidine)

Mechanism of action

H2-receptor antagonist; blocks H2-receptors of gastric parietal cells, leading to inhibition of gastric secretions

 

Pharmacokinetics

Half-Life: 2.5-3hr (PO); 2-2.5hr (IV)

Peak Plasma Time: 2-3hr (PO); <15 min (IM)

Absorption: 50% (oral)

Bioavailability: 48-50% (PO); 90-100% (IM)

Protein Bound: 15%

Vd: 0.8-1.5 L/kg

Metabolism: Liver, unlike cimetidine, nizatidine does not inhibit microsomal enzymes

Metabolites: N-desmethylnizatidine (active), nizatidine N-oxide (inactive), nizatidine S-oxide (inactive)

Dialyzable: No

Clearance

  • Total Body: 660-1000 mL/min
  • Renal: 500 mL/min (Not dialyzable by HD)

Excretion

  • Urine: 30% (PO); 70% (IV)
  • Feces: <6%