The drug that is most commonly used for treatment of obesity is sibutramine.
DRUG CLASS AND MECHANISM
It is the drug of class appetite suppressants, also called serotonin-nor epinephrine reuptake inhibitors, that works by acting on control centers in the brain that controls the appetite. The drug decreases appetite by blocking the reuptake of neurotransmitters that is dopamine, nor epinephrine and serotonin. This alters their balance within the nerve cells thereby affecting the nerve function and interaction.
AVAILABLE DOSAGE FORMS
Capsules, 5mg (blue and yellow), 10mg (blue and white), 15mg (white and yellow). BRAND NAMEs, Reductil, Meridia, Sibutrex. STORAGE CONDITIONS, Capsules should be stored at 25°C (77°F), A tight, light-resistant container should be used for their storage. The capsules should be protected from heat and moisture.
INDICATED USE. This drug is used for losing weight along with a well balanced and low caloric diet. It is indicated for people with an initial body mass index of more than 30 kg/m2 or if they also have other risk factors such as diabetes mellitus, high cholesterol or hypertension than it is 27 mg/m2.
DOSING: Sibutramine is taken once daily, generally in the morning. Initially the therapy is started with one 10mg tablet per day. The dose may be increased to achieve the desired effect upto 15mg by the physician after several weeks. Sibutramine may be taken with or without food.
DRUG INTERACTIONS:
In the liver Sibutramine is converted to its active form.
This conversion is inhibited by, Ketoconazole (Nizoral), Cimetidine (Tagamet), Erythromycin (Erytab, Eryc, Ilosone), clarithromycin (Biaxin), danazol (Danocrine), diltiazem (Cardizem, Tiazac, Dilacor), fluconazole (Diflucan), fluoxetine (Prozac), itraconazole (Sporanox), propoxyphene (Darvon), troleandomycin (Tao) verapamil (Verelan, Covera, Calan, Isoptin).
A decreased conversion and effectiveness of sibutramine can result if these are used with sibutramine.
Serotonin syndrome may appear in people who take sibutramine along with a) Selective serotonin reuptake inhibitors (SSRIs) such as, fluoxetine (Prozac), fluvoxamine (Luvox), paroxetine (Paxil), sertraline (Zoloft)b) monoamine oxidase inhibitor drugs (MAO inhibitors) such as, Selegiline (Deprenyl, Eldepryl, Emsam), Hydralazine (Apresoline)Isoniazid (Laniazid, Nydrazid)
The serotonin syndrome may include these symptoms anxiety, dizziness, confusion, excessive sweating, shivering, fast heart rate, tremor, disorientation, vomiting, excitement, fever, loss of coordination, loss of consciousness, and weakness. Serotonin syndrome can also be caused if sibutramine is used with medications used for migraines such as sumatriptan (Imitrex), zolmitriptan (Zomig) and dihydroergotamine (DHE), dextromethorphan in many cough medications such as Robitussin-DM, meperidine (Demerol), pentazocine (Talwin) and fentanyl (Duragesic), or lithium (Eskalith).
These drugs should not be used with sibutramine as they can cause life threatening problems. So it is better not to use sibutramine and drugs from any of these classes of drugs. If required the minimum interval between takings the drugs from either class or sibutramine should be at least 2 weeks.
PREGNANCY AND NURSING MOTHERS:
As there is no evidence that sibutramine can cause any harm to the fetus, thus the use is not recommended. Women should use contraception if there is any chance of becoming pregnant.
It is not known whether sibutramine or its active products accumulate in breast milk. Sibutramine, therefore, is also not recommended for nursing mothers.
SIDE EFFECTS:
Sibutramine is well-tolerated but it can cause some unwanted effects. Blood pressure and pulse may be measured and laboratory tests performed to monitor side effects. The most common side effects have been constipation, insomnia, headache, and dry mouth. Other less common side effects include abdominal pain, acne, rash, chest pain, anxiety, joint pain, back pain, excitation, depression, sweating, dizziness, drowsiness, changes in taste, irregular or painful menstrual periods, flu-like syndrome, increased cough, muscle pain, nausea, vomiting, and neck pain, nervousness, tingling of the extremities, sore throat, and sinus congestion.
Abnormal liver tests have also been reported.
Depression, psychosis, mania, suicidal thoughts and suicide have been rarely reported during treatment however, sibutramine as the cause has not been established. Sibutramine probably should be discontinued in case of any of these events occur during treatment.
OVERDOSE OR MISSED DOSE:
Symptoms of overdose may include fast heartbeat. If it is suspected contact your local poison control center or emergency room immediately. In case of a missed dose, the dose should be taken as soon as you remember. But if it is near the second dose skip the missed dose and take the regular dosing schedule. Remember that it is not a good choice to double the dose if dose is missed.
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