Phendimetrazine (Bontril) - Uses, Dose, MOA, Brands, Side effects

Phendimetrazine is a sympathomimetic amine, which means it's a stimulant that affects the central nervous system. It is used as a short-term adjunct in the management of obesity, along with dietary and lifestyle modifications. It's typically prescribed when other weight loss efforts have failed. Phendimetrazine works by decreasing appetite, increasing metabolism, and affecting certain areas of the brain that control hunger.

Phendimetrazine (Bontril) is an anorectic drug similar to amphetamines. It suppresses appetite and increases the metabolic rate. It is used in the management of exogenous obesity as an adjunct to diet and exercise.

Phendimetrazine Uses:

  • Obesity:
    • It is used in the management of obesity as a short-term treatment in adjunct to a low caloric diet and exercise.

Phendimetrazine (Bontril) Dose in Adults

Phendimetrazine (Bontril) Dose in the short-term treatment of Obesity: Oral: 

Phendimetrazine to help with weight loss for a short time, there are two ways to take it by mouth:

  • Extended-release tablets:
    • You take 105 milligrams just once every day, about 30 to 60 minutes before eating breakfast in the morning.
  • Immediate-release tablets:
    • You take 35 milligrams either 2 or 3 times a day, depending on what your doctor recommends.
    • Take it about an hour before meals.
    • Sometimes, you might only need half a tablet (17.5 milligrams) per dose.
    • But don't take more than 70 milligrams three times a day.

Phendimetrazine (Bontril) Dose in Children:

Refer to adults dosing.

Pregnancy Risk Factor X/C

  • The risk of using Phendimetrazine during pregnancy is uncertain (Risk Factor X/C).
  • Studies on pregnant animals haven't been done, but some manufacturers advise against using it during pregnancy because it might not benefit the mother and could potentially harm the baby.
  • It's important to note that being overweight during pregnancy can increase the chances of problems for both the mother and the baby.
  • However, medications like Phendimetrazine aren't recommended for weight loss during pregnancy or when planning to conceive, according to the American College of Obstetricians and Gynecologists.

Use during breastfeeding:

  • It's not clear if Phendimetrazine passes into breast milk, but similar drugs called amphetamines have been found in breast milk before.
  • Because there's a chance of harmful effects on the baby who is breastfeeding, it's important to think about whether to stop breastfeeding or stop taking the medication, depending on how important the drug is for the mother.
  • Some manufacturers advise against using Phendimetrazine while breastfeeding.

Dose in Kidney Disease:

  • The manufacturer's instructions don't mention any specific changes in dosage for people with kidney problems because this hasn't been studied.
  • However, since Phendimetrazine is eliminated from the body through the kidneys, it's important to be cautious when using it if you have kidney issues.

Dose in Liver Disease:

  • The manufacturer's instructions don't include any specific changes in dosage for individuals with liver problems.
  • However, if you have liver issues, it's important to discuss this with your doctor before taking Phendimetrazine.

Side effects of Phendimetrazine (Bontril):

  • Cardiovascular:
    • Flushing
    • Hypertension
    • Ischemic Events
    • Palpitations
    • Tachycardia
    • Valvular Disease (Regurgitant)
  • Central Nervous System:
    • Agitation
    • Dizziness
    • Headache
    • Insomnia
    • Overstimulation
    • Psychosis
    • Restlessness
  • Endocrine & Metabolic:
    • Changes In Libido
  • Gastrointestinal:
    • Constipation
    • Diarrhea
    • Nausea
    • Stomach Pain
    • Xerostomia
  • Genitourinary:
    • Dysuria
    • Urinary Frequency
  • Neuromuscular & Skeletal:
    • Tremor
  • Ocular:
    • Blurred Vision
    • Mydriasis
  • Respiratory:
    • Primary Pulmonary Hypertension
  • Miscellaneous:
    • Diaphoresis
    • Tachyphylaxis

Contraindications to Phendimetrazine (Bontril):

Phendimetrazine is not recommended for individuals who have a hypersensitivity or idiosyncrasy to phendimetrazine, other similar stimulant medications, or any of its components. It should also be avoided in people with conditions like glaucoma, severe nervousness, history of drug abuse, or hyperthyroidism. Taking Phendimetrazine along with other weight loss medications or CNS stimulants is not advised. Additionally, it should not be taken during or within 14 days following therapy with monoamine oxidase inhibitors (MAOIs).

  • Extended-release Phendimetrazine is further contraindicated in individuals with a history of cardiovascular disease, pregnancy, or breastfeeding.
  • Immediate-release Phendimetrazine is not recommended for those with advanced arteriosclerosis, symptomatic cardiovascular disease, or moderate to severe hypertension. These contraindications aim to prevent potential adverse effects and complications.

Warnings and precautions

CNS depression:

  • Phendimetrazine may lead to CNS depression, which can affect physical and mental abilities.
  • Patients should be careful when performing tasks requiring alertness like driving or operating machinery.

Heart failure:

  • According to the American Heart Association, Phendimetrazine has been linked to potential myocardial toxicity, which can seriously affect the heart.

Hypertension in the lungs:

  • Although rare, pulmonary hypertension may occur and can be fatal.
  • Prolonged use of this medication for more than three months raises the risk.
  • Seek medical attention if symptoms like difficulty breathing or chest pain occur.

Heart disease of the valvular kind:

  • Long-term use or high doses of Phendimetrazine, especially when combined with other weight loss drugs, may contribute to valvular heart disease.
  • Avoid use in individuals with known heart murmurs or valvular issues.

Diabetes:

  • Caution is advised in patients with diabetes as Phendimetrazine may alter the requirements for diabetes medications due to dietary changes and appetite suppression.

Hypertension:

  • Patients with hypertension or other heart conditions should use Phendimetrazine cautiously as it can increase blood pressure and heart rate.

Renal impairment

  • Use caution in patients with kidney problems.

Seizure disorders:

  • Individuals with a history of seizures should be cautious when using Phendimetrazine.

Tourette syndrome:

  • Patients with Tourette syndrome should use Phendimetrazine cautiously as stimulants might worsen tic symptoms.

Phendimetrazine: Drug Interaction

Risk Factor C (Monitor therapy)

Alcohol (Ethyl)

May enhance the adverse/toxic effect of Phendimetrazine.

Amifampridine

Agents With Seizure Threshold Lowering Potential may enhance the neuroexcitatory and/or seizure-potentiating effect of Amifampridine.

Ammonium Chloride

May decrease the serum concentration of Amphetamines. This effect is likely due to an enhanced excretion of amphetamines in the urine.

Antacids

May decrease the excretion of Amphetamines.

Antihistamines

Amphetamines may diminish the sedative effect of Antihistamines.

Antihypertensive Agents

Amphetamines may diminish the antihypertensive effect of Antihypertensive Agents.

Antipsychotic Agents

May diminish the stimulatory effect of Amphetamines.

Ascorbic Acid

May decrease the serum concentration of Amphetamines.

AtoMOXetine

May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics.

BuPROPion

May enhance the neuroexcitatory and/or seizure-potentiating effect of Agents With Seizure Threshold Lowering Potential.

Cannabinoid-Containing Products

May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol.

Carbonic Anhydrase Inhibitors

May decrease the excretion of Amphetamines. Exceptions: Brinzolamide; Dorzolamide.

CYP2D6 Inhibitors (Moderate)

May increase the serum concentration of Amphetamines.

CYP2D6 Inhibitors (Strong)

May increase the serum concentration of Amphetamines.

Doxofylline

Sympathomimetics may enhance the adverse/toxic effect of Doxofylline.

Esketamine

May enhance the hypertensive effect of CNS Stimulants.

Ethosuximide

Amphetamines may diminish the therapeutic effect of Ethosuximide. Amphetamines may decrease the serum concentration of Ethosuximide.

Gastrointestinal Acidifying Agents

May decrease the serum concentration of Amphetamines.

Guanethidine

May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics.

Ioflupane I 123

Amphetamines may diminish the diagnostic effect of Ioflupane I 123.

Lithium

May diminish the stimulatory effect of Amphetamines.

Methenamine

May decrease the serum concentration of Amphetamines. This effect is likely due to an enhanced excretion of amphetamines in the urine.

Multivitamins/Fluoride (with ADE)

May decrease the serum concentration of Amphetamines. More specifically, the ascorbic acid (vitamin C) in many multivitamins may decrease amphetamine concentrations.

Multivitamins/Minerals (with ADEK, Folate, Iron)

May decrease the serum concentration of Amphetamines.

Multivitamins/Minerals (with AE, No Iron)

May decrease the serum concentration of Amphetamines. Specifically, vitamin C may impair absorption of amphetamines.

Opioid Agonists

Amphetamines may enhance the analgesic effect of Opioid Agonists.

PHENobarbital

Amphetamines may decrease the serum concentration of PHENobarbital.

Phenytoin

Amphetamines may decrease the serum concentration of Phenytoin.

Solriamfetol

Sympathomimetics may enhance the hypertensive effect of Solriamfetol.

Solriamfetol

CNS Stimulants may enhance the hypertensive effect of Solriamfetol.

Sympathomimetics

May enhance the adverse/toxic effect of other Sympathomimetics.

Tedizolid

May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics.

Tricyclic Antidepressants

May enhance the stimulatory effect of Amphetamines. Tricyclic Antidepressants may also potentiate the cardiovascular effects of Amphetamines.

Urinary Acidifying Agents

May decrease the serum concentration of Amphetamines.

Risk Factor D (Consider therapy modification)

Alkalinizing Agents

May decrease the excretion of Amphetamines. Management: Consider alternatives to using amphetamines and alkalinizing agents in combination. If these agents must be used together, patients should be monitored closely for excessive amphetamine effects.

Cocaine (Topical)

May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use.

Iohexol

Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iohexol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iohexol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants.

Iomeprol

Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iomeprol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iomeprol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants.

Iopamidol

Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iopamidol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iopamidol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants.

Linezolid

May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available.

Risk Factor X (Avoid combination)

Acebrophylline

May enhance the stimulatory effect of CNS Stimulants.

Iobenguane Radiopharmaceutical Products

Amphetamines may diminish the therapeutic effect of Iobenguane Radiopharmaceutical Products. Management: Discontinue all drugs that may inhibit or interfere with catecholamine transport or uptake for at least 5 biological half-lives before iobenguane administration. Do not administer these drugs until at least 7 days after each iobenguane dose.

Iobenguane Radiopharmaceutical Products

CNS Stimulants may diminish the therapeutic effect of Iobenguane Radiopharmaceutical Products. Management: Discontinue all drugs that may inhibit or interfere with catecholamine transport or uptake for at least 5 biological half-lives before iobenguane administration. Do not administer these drugs until at least 7 days after each iobenguane dose.

Monoamine Oxidase Inhibitors

May enhance the hypertensive effect of Amphetamines. While linezolid and tedizolid may interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to monographs specific to those agents for details. Exceptions: Linezolid; Tedizolid.

Sibutramine

May enhance the adverse/toxic effect of Centrally Acting Weight Loss Agents.

Monitoring Parameters:

Baseline Cardiac Evaluation:

  • Before starting Phendimetrazine, patients should undergo a cardiac evaluation to assess for preexisting conditions like valvular heart disease or pulmonary hypertension.

Echocardiogram During Therapy:

  • Regular echocardiograms should be performed during Phendimetrazine therapy to monitor cardiac function and detect any potential complications.

Monitoring Weight and Waist Circumference:

  • Regularly monitor weight and waist circumference to track progress and ensure safe use of Phendimetrazine.

Blood Pressure Monitoring:

  • Monitor blood pressure regularly, especially in patients with hypertension or cardiovascular conditions, to detect any changes or exacerbation of existing conditions.

How to administer Phendimetrazine (Bontril)?

Extended-Release:

  • Take the extended-release formulation of Phendimetrazine 30 to 60 minutes before your morning meal.

Immediate-Release:

  • Take the immediate-release formulation of Phendimetrazine 1 hour before your meals.

Mechanism of action of Phendimetrazine (Bontril):

  • Phendimetrazine is a type of drug called a sympathomimetic amine, which works in a way similar to amphetamines.
  • It seems to reduce appetite by affecting the central nervous system (CNS).
  • Specifically, it stimulates a part of the brain called the hypothalamus to release a chemical called norepinephrine, which helps control appetite.
  • This action in the brain is what helps people feel less hungry when they take Phendimetrazine.

Metabolism:

  • Phendimetrazine undergoes metabolism in the body, forming two metabolites: phenmetrazine and phendimetrazine-N-oxide.

Half-life elimination:

  • The half-life of Phendimetrazine, which is the time it takes for half of the drug to be eliminated from the body, is approximately 3.7 hours.

Excretion:

  • After metabolism, Phendimetrazine and its metabolites are primarily excreted through urine.

International Brand Names of Phendimetrazine:

  • Bontril PDM
  • Anoran
  • Antapentan
  • Atrajine
  • Fendy 35
  • Furing
  • Obesan-X
  • Pendimen
  • Phendirazine
  • Plegine
  • Prelu-2

Phendimetrazine Brand Names in Pakistan:

No Brands Available in Pakistan.

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