Mesalazine

BRAND NAMES:

Apriso – It contains the active ingredient of mesalamine. It is available as extended-release capsules used to treat bowel conditions.

Asacol HD- It contains the active ingredients of mesalamine. It is available as delayed-release tablets used to treat ulcerative colitis.

Delzicol – It contains the active ingredient of mesalamine. It is available in the form of delayed-release capsules.

MECHANISM OF ACTION:

It is thought to have a topical anti-inflammatory action on colonic epithelial cells. Patients with chronic inflammatory bowel disease have increased mucosal production of arachidonic acid metabolites via the cyclooxygenase pathway, which produces prostanoids, and the lipoxygenase pathway, which produces leukotrienes and hydroxy eicosatetraenoic acids, and it is possible that mesalazine reduces inflammation by inhibiting cyclooxygenase and prostaglandin production in the colon.

 PHARMACOKINETICS:

Absorption: The amount of mesalazine absorbed from oral delayed-release tablets (2.4g or 4.8g) given to healthy volunteers once daily for 14 days was between 21% and 22% of the administered dose, depending on the formulation. On the other hand, the amount of mesalazine absorbed from oral controlled-release capsule formulations was found to be between 20% and 30% of the formulation.

Distribution: Mesalazine's Vd of 18L for the extended-release formulation confirms that the systemically accessible medication has low extravascular penetration. The apparent volume of distribution for the delayed-release formulation was calculated to be 4.8 liters.

Metabolism: Mesalazine is metabolized into N-acetyl-5-aminosakicylic acid, primarily via NAT-1, both pre-systemically by the intestinal mucosa and systemically in the liver. Additionally, some acetylation is produced by intestinal bacteria.

Excretion: Mesalazine is primarily eliminated by the kidneys after metabolization into N-acetyl-5-aminosalicylic acid. The parent medication mesalazine is likewise excreted in small amounts in the urine.

PHARMACODYNAMICS:

Mesalazine is hypothesized to reduce inflammation by inhibiting prostaglandin synthesis, interfering with leukotriene synthesis and hence leukocyte migration, and acting as a powerful free radical scavenger. Regardless of the course of action. Mesalazine appears to be active mostly topically, rather than systemically.

DOSAGE AND ADMINISTRATION:

Mesalazine is available in the form of capsules and tablets taken orally with the following strengths

• Extended-release capsules – 250mg, 375mg, and 500mg.

• Delayed release tablets –1.2gr

• Delayed release capsules- 400mg

Mesalazine is available as a delayed-release tablet, a delayed-release capsule, and an extended-release capsule to be taken orally. Adults and children typically take delayed-release pills with food once per day. Adults often take delayed-release pills three times per day, on an empty stomach. Adults commonly take extended-release capsules with or without meals in the morning. Adults often take extended-release capsules with or without food four times per day. Adults often take extended-release capsules with or without meals 2 to 4 times per day, while children take them twice a day, preferably in the morning and afternoon.

DRUG INTERACTIONS:

Drug interactions with mesalazine may include

• NSADs – aspirin and ibuprofen

• Immuno supressants – azathioprine

CONTRAINDICATIONS:

Patients with salicylate or component hypersensitivity, as well as significant renal impairment, should not take this medication. Serious blood dyscrasias have been documented seldom with mesalazine. It is contraindicated in cases of severe hepatic impairment.

SIDE EFFECTS:

• Muscle or joint pains

• Back pain

• Nausea

• Vomiting

• Heartburn

• Burping

• Constipation

• Gas

• Itching

• Dizziness

• Hair loss

• Runny nose

Some serious side effects may include

• Rash
• Mouth sores
• Fever
• Chest pain
• Shortness of breath
• Bloody vomit
• Vomiting
• Side or back pain
• Extreme tiredness
• Yellowing of the skin or eyes
• Pale stools
• Pain in the right upper part of the stomach 

OVERDOSE:

Symptoms of overdose may include

• Nausea, vomiting and abdominal pain

• Fast or shallow breathing

• Headache

• Dizziness

• Seizures

• Confusions

 TOXICITY:

There is no particular antidote for mesalazine overdose, however normal salicylate treatment may be effective. This may involve decontaminating the gastrointestinal system, replenishing fluids and electrolytes, and preserving renal function.