Nobese Sibutramine HCL 15 mg-Pharmasltd

Description

Nobese, manufactured by Getz Pharma, is an orally administered serotonin and noradrenaline reuptake inhibitor (SNRI) used for the management of obesity. Its chemical name is Sibutramine Hydrochloride.

Nobese works by reducing body weight through dual actions: enhancing satiety to decrease food intake and increasing energy expenditure through thermogenesis. It primarily achieves these effects by inhibiting the reuptake of serotonin and noradrenaline.

When taken orally, Nobese is rapidly absorbed from the gastrointestinal tract. The peak plasma concentration of the parent drug occurs after approximately 1.2 hours, while the active metabolites M1 and M2 reach their peak concentrations after three to four hours. On average, at least 77% of a single oral dose of Nobese is absorbed.

Both Nobese and its metabolites M1 and M2 are extensively bound to human plasma proteins (97% and 94% respectively). The drug is widely distributed in renal and hepatic tissues.

Nobese undergoes significant first-pass metabolism. It is primarily metabolized by the enzyme cytochrome P450 isoenzyme CYP3A4, resulting in the formation of two active metabolites, secondary and primary amine metabolites. These active metabolites undergo further metabolism through hydroxylation and conjugation to produce inactive M5 and M6 metabolites.

The main route of excretion for the active metabolites is hepatic metabolism, while the inactive metabolites are excreted through the kidneys. The elimination half-life of Nobese in plasma is approximately 14-16 hours.

In patients with moderate hepatic impairment, the combined exposure (AUC) of the active metabolites M1 and M2 may increase by 24% after a single 15 mg oral dose of Nobese. However, this increase does not typically warrant a dose adjustment.

Renal insufficiency may affect the elimination of the inactive hydroxyl metabolites, which are primarily excreted by the kidneys.

Nobese is indicated for the management of obesity, including weight loss and weight maintenance, when used in conjunction with a reduced-calorie diet. It is specifically recommended for patients with an initial body mass index (BMI) of less than 30 kg/m² or less than 27 kg/m² in the presence of other risk factors such as hypertension, diabetes, or dyslipidemia.

The recommended initial oral dose of Nobese is a 10 mg capsule once daily, with or without food. If there is insufficient weight loss (less than 20 kg), the dose may be increased to 15 mg, provided that the 10 mg dose was well tolerated. The 5 mg dose should be reserved for patients who cannot tolerate the 10 mg dose.

Treatment with Nobese should not exceed one year. Maximum weight loss (5%-10% of initial body weight) is typically achieved within six months. If a patient’s weight loss stabilizes at less than 5% of their initial body weight or if their weight loss is less than 5% within three months of starting therapy, Nobese should be discontinued. Additionally, if a patient regains 3 kg or more after previously achieved weight loss, Nobese should not be continued.

Adverse reactions to Nobese are most commonly observed during the initial four weeks of treatment. The severity and frequency of these reactions generally decrease over time. Commonly observed adverse events include dry mouth, headache, insomnia, constipation, diarrhea, back pain, increased appetite, dizziness, influenza-like symptoms, and rhinitis.

Less frequent adverse reactions with Nobese include dyspepsia, nausea, dysmenorrhea, increased sweating and thirst, edema, paresthesia, taste perversion, d

rowsiness, skin rashes, palpitations, vasodilation, anxiety, nervousness, and depression.

Rare adverse reactions with Nobese include abnormal bleeding (including Henoch-Schonlein purpura), thrombocytopenia, acute interstitial nephritis, glomerulonephritis, emotional lability, seizures, blurred vision, gallstone formation, and reversible increase in liver enzymes.