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Nizatidine

Drug Approvals

(British Approved Name, US Adopted Name, rINN)

NizatidineSynonyms: LY-139037; Nitsatidiini; Nizatidin; Nizatidina; Nizatidinas; Nizatidinum; ZL-101
BAN: Nizatidine
USAN: Nizatidine
INN: Nizatidine [rINN (en)]
INN: Nizatidina [rINN (es)]
INN: Nizatidine [rINN (fr)]
INN: Nizatidinum [rINN (la)]
INN: Низатидин [rINN (ru)]
Chemical name: 4-[2-(1-Methylamino-2-nitrovinylamino)ethylthiomethyl]thiazol-2-ylmethyl(dimethyl)amine; N-[2-(2-Dimethylaminomethylthiazol-4-ylmethylthio)ethyl]-N´-methyl-2-nitrovinylidenediamine
Molecular formula: C12H21N5O2S2 =331.5
CAS: 76963-41-2
ATC code: A02BA04
Read code: y01QF

Pharmacopoeias. In Europe and US.

European Pharmacopoeia, 6th ed. (Nizatidine). An almost white or slightly brownish, crystalline powder. Sparingly soluble in water soluble in methyl alcohol. A 1% solution in water has apH of 8.5 to 10.0.

The United States Pharmacopeia 31, 2008 (Nizatidine). An off-white to buff crystalline solid. Sparingly soluble in water freely soluble in chloroform soluble in methyl alcohol. Store in airtight containers. Protect from light.

Adverse Effects

As for Cimetidine. Some patients taking nizatidine may experience excessive sweating and urticaria anaemia may also occur.

Nizatidine is considered to have little or no anti-androgenic activity although there are isolated reports of gynaecomastia and impotence.

Effects on the cardiovascular system

Nizatidine has been reported to reduce heart rate in healthy subjects, an effect that was not seen when they were pretreated with ranitidine or also given the antimuscarinic pirenzepine. As with other H2-antagonists (see Cimetidine), tachycardia, bradycardia, orthostatic hypotension and syncope have been reported rarely with rapid intravenous injection of nizatidine.

Effects on the endocrine system

A report of reversible impotence in a patient taking nizatidine 300 mg at night.

Effects on the skin

Similarly to cimetidine, vasculi-tis has been reported with nizatidine. Exfoliative dermatitis has also occurred.

Precautions

As for Cimetidine.

Interactions

Unlike cimetidine nizatidine does not inhibit cytochrome P450, and therefore is considered to have little effect on the metabolism of other drugs. However, like other H2-antagonists its effects on gastric pH may affect the absorption of some other drugs.

Pharmacokinetics

Nizatidine is readily and almost completely absorbed from the gastrointestinal tract. The bioavailability of nizatidine after oral doses exceeds 70% and may be slightly increased by the presence of food. It is widely distributed and is about 35% bound to plasma proteins. The elimination half-life of nizatidine is 1 to 2 hours and is prolonged in renal impairment. Nizatidine is partly metabolised in the liver: nizatidine N-2-oxide, nizatidine S-oxide, and N-2-monodesmethylnizatidine have been identified, the latter having about 60% of the activity of nizatidine.

More than 90% of a dose of nizatidine is excreted in the urine, in part by active tubular secretion, within 12 hours, about 60% as unchanged drug. Less than 6% is excreted in the faeces. Nizatidine is distributed into breast milk.

Bioavailability

The bioequivalence of 3 oral liquid formulations of nizatidine was investigated relative to a commercially available nizatidine capsule. Of the 3 liquid formulations, one was a commercially available oral syrup (15 mg/mL), and 2 others were extemporaneously prepared, one as a solution in apple juice (1.2 mg/mL) and another as a suspension in an infant formula (Erfamil Ross, USA: 15 mg/mL). Nizatidine in apple juice showed markedly less bioavailability, whereas the other 2 formulations were considered to be bioequivalent to the reference capsule.l

Distribution into breast milk

About 0.1% of an oral dose of nizatidine was secreted in breast milk in a study in lactating women. The milk to serum ratio varied (from 1:1 to 4.9:1) with the time of samples.

Uses and Administration

NizatidineNizatidine is a histamine H2-antagonist with actions and uses similar to those of cimetidine. It is given orally and by intravenous infusion. In the management of benign gastric and duodenal ulceration a single daily oral dose of nizatidine 300 mg at night is recommended, which should be given initially for 4 weeks and may be extended to 8 weeks if necessary alternatively 150 mg may be given twice daily in the morning and evening.

Where appropriate a maintenance dose of 150 mg daily may be given at night. In patients who are unsuited to receive oral therapy nizatidine may be given on a short-term basis by continuous intravenous infusion of 10 mg/hour alternatively 100 mg may be diluted in 50 inL of infusion fluid and be given over 15 minutes, three times daily. The total intravenous dose should not exceed 480 mg daily.

In gastro-oesophageal reflux disease an oral dose of 150 to 300 mg twice daily is recommended for up to 12 weeks. In children aged 12 years and older, a dose of 150 mg twice daily may be given for up to 8 weeks.

For the short-term symptomatic relief of dyspepsia a dose of 75 mg, repeated if necessary, up to a maximum of 150 mg daily may be taken by mouth for up to 14 days.

Doses of nizatidine should be reduced in patients with renal impairment.

Administration in renal impairment

The dosage of nizatidine should be reduced in patients with renal impairment according to creatinine clearance (CC). Licensed product information recommends the following oral doses in renal impairment:

  • CC 20 to 50 mL/minute: doses should be reduced by 50%, or where the standard dose would be 150 mg daily, 150 mg may be given on alternate days
  • CC less than 20 mL/minute: doses should be reduced by 75%, or where the standard dose would be 300 mg daily, 150 mg may be given on alternate days, and where the standard dose would be 150 mg daily, 150 mg may be given every third day

Preparations

British Pharmacopoeia 2008: Nizatidine Intravenous Infusion

The United States Pharmacopeia 31, 2008: Nizatidine Capsules.

Proprietary Preparations

Australia: Nizac Tacidine Tazac

Austria: Ulxit

Belgium: Panaxid

Brazil: Axid

Canada: Axid

Chile: Nizaxid

Denmark: Izatax Nizax

Finland: Nizax

France: Nizaxid

Germany: Gastrax Nizax

Greece: Axidf Flectar Flexidon Ozeltan Ulcogastrin

Hong Kong: Axid

Hungary: Naxidin

Indonesia: Axid

Ireland: Axid

Italy: Cronizat Nizax Zanizal

Malaysia: Axid

Mexico: Axid Uldadin

The Netherlands: Axid

Philippines: Axid

Portugal: Nizaxid Prospaxid

South Africa: Antizid

Spain: Distaxid

Sweden: Nizax

Switzerland: Calmaxid

Thailand: Axid

Turkey: Axid

UK: Axid

USA: Axid

Venezuela: Axid

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