GACET – 125 mg / 250 mg / 500 mg / 1 g Acetaminophen Suppositories USP

Composition

Gacet 125 mg / 250 mg

Each suppository contains:

• Acetaminophen USP 125 mg / 250 mg
• Excipients
• Colour: Titanium Dioxide BP

Gacet 500 mg / 1 g

Each suppository contains:

• Acetaminophen USP 500 mg / 1 g
• q.S.
• Excipients
• q.s.

Pharmacology

The mechanism of action: Until recently, Acetaminophen was supposed to have predominantly a strong inhibitory action on prostaglandin production in the central nervous system. The rank of this mechanism has been questioned recently, and several other findings have been published: an interaction with bulbospinal pathways, inhibition of spinal substance P-mediated analgesia, and a reduction of nitric oxide generation involved in spinal hyperalgesia.

Furthermore, an inhibition of DNA repair by Acetaminophen was reported which may contribute to its clastogenic effects.

Pharmacokinetics

Acetaminophen is well absorbed by both oral and rectal routes.

Peak plasma concentrations occur about 2 to 3 hours after rectal administration. The plasma half life is about 2 hours

Acetaminophen is primarily metabolized in the liver by conjugation to glucuronide and sulphate. A small amount (about 3-10% of a therapeutic dose) is metabolized by oxidation and the reactive intermediate metabolite thus formed is bound preferentially to the liver glutathione and excreted as cystein and mercapturic acid conjugates. Excretion occurs via the kidneys. 2-3% of a therapeutic dose is excreted unchanged: 80-90% as glucoside and sulphate and a smaller amount as cysteine and mercapturic acid derivatives.

Indications

Symptomatic relief of pain and fever

• Gacet -125 Suppository:
  1 - 5 years (10 - 20kg): 1 - 2 suppositories

• Gacet -250 Suppository:
  6 - 12 years (20 - 40kg): 1 - 2 Suppositories

• Gacet -500 Suppository:
  Children over 12 years and adults (40 kg and above): 1 - 2 Suppositories

• Gacet -1g Suppository:
  Adults and children > 40 kg: 1 suppository

Contraindications

• Known allergy to Acetaminophen
• Serious liver disorder
• Rectal bleeding or inflammation (contraindication related directly to the administration route of the medicine)

Precautions and Warning

Acetaminophen should be given with care to patients with impaired liver or kidney function. In the event of uric acid or sugar content tests, the patient should be advised to disclose the intake of Acetaminophen. If the pain persists for more than 5 days or the fever for more than 3 days, or in the event of aggravation, treatment should not be continued without seeking advice serious illness from the doctor. Severe or recurrent pain or high or continued fever may be indicative of

Pregnancy and Lactation

Epidemiological studies in human pregnancy have shown no ill effects due to Paracetamol regarding its use used in the recommended dosage, but patient should follow the advice of their doctor Paracetamol is excreted in breast milk but not in clinically significant amount. Available published data do not contraindicate breast feeding.

Interactions

The medicine contains Acetaminophen. It should not be combined with other Acetaminophen preparations so as not to exceed recommended daily dose.

Drugs which include hepatic microsomal enzymes such as alcohol, Rifampicin, barbiturates and other anti-convulsants may increase the hepatotoxicity of Acetaminophen particularly after overdosage. The therapeutic effects of Acetaminophen may also be decreased.

Adverse Reactions

If used as directed, Acetaminophen rarely causes severe toxicity or side effects. In some rare cases a cutaneous eruption or an allergic reaction may occur. Redness of the mucous membrane of the rectum and minor local vascular changes may be reported. Hepatic necrosis may occur after overdosage.

Reasons for immediate discontinuation of the drug

• Exceptional biological changes requiring a blood analysis.
• Abnormally low count of certain blood constituents (platelets)
• Local effects related to administration route. These are all the more frequent and severe if the duration of treatment is prolonged and the frequency of intake and the dosage are high.

Overdosage

In the event of overdosage or accidental ingestion of a very high dose (150mg/kg), the doctor should be immediately consulted. Specific antidote is N Acetyl Cysteine.

Excipients

• Gacet 125 mg / 250 mg:
  Polyethylene glycol 1500 BP, Polyethylene glycol 6000 BP, Methyl Paraben BP, Propyl Paraben BP, Butylated Hydroxytoluene BP, Titanium Dioxide BP

• Gacet 500 mg / 1g:
  Hard Fat BP

Administration Route

For rectal administration only.
Not to be taken orally.

Storage

Store in the original package below 30°C.
Keep out of the reach and sight of children.

Presentations

• Pack of 2 x 5 Suppositories
• Pack of 20 x 5 Suppositories
• Pack of 5 Suppositories

How to Use Suppository

• When practical, clean the area around the rectum with mild soap and warm water and rinse thoroughly. Gently dry by patting or blotting with toilet tissue
• Do not open suppository if it seems soft, hold the foil wrapper under cold water or place it in refrigerator for few minutes to harden it before removing
• Position the patient to lie on one side with knees bent up to their abdomen or lie on back with feet and legs held up.
• Wash your hands and detach the suppository by holding strip upright and if dry) carefully peel the wrapper evenly down both sides. (moisten the suppository
• Hold the suppository between index finger and thumb, locate the anus and gently insert suppository tip end first with the index finger. The suppository should be fully inserted in to rectum against the wall of rectum.
• Hold buttocks together lying down for about 5 minutes to avoid having the suppository comes out.
• Discard used materials and wash your hands thoroughly.

Date of Publication / Review

December 2017

Manufacturer

Bliss
Míd. by: BLISS VS PHARMA LTD.
Dewan Udyog Nagar, Aliyali, Palghar, Maharashtra - 401 404, INDIA.
Regd. Off. 102, Hyde Park, Saki Vihar Road, Andheri (E), Mumbai - 400 072, INDIA.