Ultrafen Plus Tablet 50 mg+200 mcg

Ultrafen Plus Tablet 50 mg+200 mcg Uses, Dosage, Side Effects, Food Interaction and all others data.

Misoprostol is a synthetic prostaglandin E1 analogue. It protects the GI mucosa by inhibiting basal, stimulated and nocturnal acid secretion and by reducing the volume of gastric secretions and increasing bicarbonate and mucus secretion. It also induces contractions of smooth muscle fibres of the myometrium and relaxation of the cervix uteri.

Misoprostol is a prostaglandin E1 analog used to reduce the risk of NSAID induced gastric ulcers by reducing secretion of gastric acid from parietal cells. Misoprostol is also used to manage miscarriages and used alone or in combination with mifepristone for first trimester abortions. An oral dose of misoprostol has an 8 minute onset of action and a duration of action of approximately 2 hours, a sublingual dose has an 11 minute onset of action and a duration of action of approximately 3 hours, a vaginal dose has a 20 minute onset of action and a duration of action of approximately 4 hours, and a rectal dose has a 100 minute onset of action and a duration of action of approximately 4 hours.

Ultrafen Plus Tablet 50 mg+200 mcg
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Ultrafen Plus Tablet 50 mg+200 mcg
Generic	Diclofenac Sodium + Misoprostol
Weight	50 mg+200 mcg
Type	Tablet
Therapeutic Class	Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
Manufacturer	Beximco Pharmaceuticals Ltd.
Available Country	Bangladesh
Last Updated:	October 19, 2023 at 6:27 am

Uses

This combination is indicated for treatment of the signs and symptoms of osteoarthritis or rheumatoid arthritis in patients at high risk of developing NSAID-induced gastric and duodenal ulcers and their complications.

Ultrafen Plus Tablet 50 mg+200 mcg is also used to associated treatment for these conditions: Gastric Ulcer, Incomplete Abortion, Missed Abortion, Postpartum Haemorrhage (PPH), Induction of cervix ripening therapy, Medically induced abortion

How Ultrafen Plus Tablet 50 mg+200 mcg works

Misoprostol is a synthetic prostaglandin E1 analog that stimulates prostaglandin E1 receptors on parietal cells in the stomach to reduce gastric acid secretion. Mucus and bicarbonate secretion are also increased along with thickening of the mucosal bilayer so the mucosa can generate new cells.

Misoprostol binds to smooth muscle cells in the uterine lining to increase the strength and frequency of contractions as well as degrade collagen and reduce cervical tone.

Dosage

Ultrafen Plus Tablet 50 mg+200 mcg dosage

Osteoarthritis: The recommended dosage for maximal GI mucosal protection is Diclofenac Sodium 50 mg & Misoprostol 200 µg tid. For patients who experience intolerance, Diclofenac Sodium 75 mg & Misoprostol 200 µg bid or Diclofenac Sodium 50 mg & Misoprostol 200 µg bid can be used.Rheumatoid arthritis: The recommended dosage is Diclofenac Sodium 50 mg & Misoprostol 200 µg tid or qid. For patients who experience intolerance, Diclofenac Sodium 75 mg & Misoprostol 200 µg bid or Diclofenac Sodium 50 mg & Misoprostol 200 µg bid can be used.

Side Effects

The most common reported side effects are abdominal pain, diarrhea and other GI symptoms. Diarrhea and abdominal pain developed early in the course of therapy and were usually self-limited (resolved after 2 to 7 days). Rare instances of profound diarrhea leading to severe dehydration have been reported in patients receiving Misoprostol.

Toxicity

The oral LD₅₀ in rats is 81mg/kg and in mice is 27mg/kg. The intraperitoneal LD₅₀ in rats is 40mg/kg and in mice is 70mg/kg.

Patients experiencing an overdose may present with sedation, tremor, convulsions, dyspnea, abdominal pain, diarrhea, fever, palpitations, hypotension, and bradycardia. Hemodialysis is not expected to be useful in the treatment of misoprostol overdose but oral activated charcoal may help reduce absorption. In the event of an overdose, treat symptoms with supportive therapy. This may include removal of undissolved tablets from the vagina or buccal cavity, intravenous fluid replacement, acetaminophen, diazepam, haloperidol, or intramuscular diclofenac depending on the symptoms that present.

Precaution

Patients with an underlying condition such as inflammatory bowel disease or those in whom dehydration should be monitored carefully if Diclofenac Sodium plus Misoprostol is prescribed.

Interaction

Aspirin: Concomitant administration with aspirin is not recommended because Diclofenac Sodium is displaced from its binding sites by aspirin, resulting in lower plasma concentrations, peak plasma levels and AUC values.Digoxin: Elevated digoxin levels have been reported in patients receiving digoxin and Diclofenac Sodium. Antihypertensives: NSAIDs can inhibit the activity of antihypertensives, including ACE inhibitors.Warfarin: The effects of warfarin and NSAIDs on GI bleeding are synergistic, such that users of both drugs together have a risk of serious bleeding greater than users of either drug alone.Oral hypoglycaemics: Diclofenac Sodium does not alter glucose metabolism in healthy people nor it alters the effects of oral hypoglycaemics. Diclofenac Sodium may alter diabetic patient’s response to insulin or oral hypoglycaemics.Antacids: Antacids reduce the bioavailability of Misoprostol. Antacids may also delay absorption of Diclofenac Sodium.Diuretics: The Diclofenac Sodium component like other NSAIDs, can inhibit the activity of diuretics. Concomitant therapy with potassium-sparing diuretics may be associated with increased serum potassium levels.

Volume of Distribution

Data regarding the volume of distribution of misoprostol is scarce.

The apparent volume of distribution of the active metabolite of misoprostol was in subjects with normal renal function was 13.6±8.0L/kg, with mild renal impairment was 17.3±23.0L/kg, with moderate renal impairment was 14.3±6.8L/kg, and with end stage renal disease was 11.0±9.6L/kg.

Elimination Route

For an 800µg oral dose of misoprostol, the AUC was 2.0192±0.8032h*ng/mL, the C_max was 2.6830±1.2161ng/mL, and a t_max of 0.345±0.186h. For a 800µg sublingual dose of misoprostol, the AUC was 3.2094±1.0417h*ng/mL, the C_max was 2.4391±1.1567ng/mL, and a t_max of 0.712±0.415h. For a 800µg buccal dose of misoprostol, the AUC was 2.0726±0.3578h*ng/mL, the C_max was 1.3611±0.3436ng/mL, and a t_max of 1.308±0.624h.

Half Life

The half life of an 800µg oral dose is 1.0401±0.5090h, for a sublingual dose is 0.8542±0.1170h, and for a buccal dose is 0.8365±0.1346h.

Clearance

Because of the rapid de-esterification of misoprostol before or during absorption, it is usually undetectable in plasma. Misoprostol's active metabolite, misoprostol acid, has a total body clearance of 0.286L/kg/min. Subjects with mild renal impairment had a total body clearance of 0.226±0.073L/kg/min, subjects with moderate renal impairment had a total body clearance of 0.270±0.103L/kg/min, and subjects with end stage renal disease had a total body clearance of 0.105±0.052L/kg/min.

Elimination Route

As much as 73.2±4.6% of a radiolabelled oral dose of misoprostol is recovered in the urine.

Pregnancy & Breastfeeding use

Because of the abortifacient property of the Misoprostol component, this is contraindicated in women who are pregnant. Diclofenac Sodium has been found in the milk of nursing mothers. Diclofenac Sodium plus Misoprostol is not recommended for use by nursing mothers.

Contraindication

This is contraindicated in patients with hypersensitivity to Diclofenac, Misoprostol or to other prostaglandins. This should not be given to patients who have experienced asthma, urticaria or other allergic-type reactions after taking aspirin or other NSAIDs.

Special Warning

Paediatric use: Safety and effectiveness of Diclofenac Sodium and Misoprostol combination in paediatric patients have not been established.Geriatric use: No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some elderly person cannot be ruled out. As with any NSAID, the elderly are likely to tolerate adverse events less well than younger patients.

Acute Overdose

Misoprostol: Convulsions, sedation, tremor, dyspnoea, diarrhoea, abdominal pain, fever, palpitations, hypotension, bradycardia. Management: Supportive treatment.Diclofenac: Lethargy, drowsiness, nausea, vomiting, epigastric pain, GI bleeding. HTN, acute renal failure, resp depression, anaphylactoid reactions and coma may occur rarely