Phendimetrazine
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Rabin Bista, M.B.B.S. [2]
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Overview
Phendimetrazine is a Appetite suppressant that is FDA approved for the treatment of exogenous obesity. Common adverse reactions include Hypertension, Tachycardia, Flushing, Sweating, Urticaria, Diarrhea, Nausea, Dizziness, Headache, Insomnia, Tremor, Agitation, Irritability, Restlessness, Dysuria.
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Indications
- Phendimetrazine tartrate tablets are indicated in the management of exogenous obesity as a short term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction. The limited usefulness of agents of this class should be measured against possible risk factors inherent in their use such as those described below.
Dosage
- 1 tablet (35 mg) b.i.d. or t.i.d., one hour before meals.
- Dosage should be individualized to obtain an adequate response with the lowest effective dosage. In some cases 1/2 tablet (17.5 mg) per dose may be adequate. * Dosage should not exceed 2 tablets t.i.d.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Phendimetrazine in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Phendimetrazine in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
- Phendimetrazine tartrate is not recommended for use in children under 12 years of age.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Phendimetrazine in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Phendimetrazine in pediatric patients.
Contraindications
- Known hypersensitivity or idiosyncratic reactions to sympathomimetics.
- Advanced arteriosclerosis, symptomatic cardiovascular disease, moderate and severe hypertension, hyperthyroidism and glaucoma.
- Highly nervous or agitated patients.
- Patients with a history of drug abuse.
- Patients taking other CNS stimulants, including Monoamine oxidase inhibitors.
Warnings
- Tolerance to the anorectic effect of phendimetrazine develops within a few weeks. When this occurs, its use should be discontinued; the maximum recommended dose should not be exceeded.
- Use of phendimetrazine tartrate within 14 days following the administration of monoamine oxidase inhibitors may result in a hypertensive crisis.
- Abrupt cessation of administration following prolonged high dosage results in extreme fatigue and depression. Because of the effect on the central nervous system, phendimetrazine may impair the ability of the patient to engage in potentially hazardous activities such as operating machinery or driving a motor vehicle; the patient should therefore be cautioned accordingly.
Precautions
- Caution is to be exercised in prescribing phendimetrazine tartrate for patients with even mild hypertension.
- Insulin requirements in diabetes mellitus may be altered in association with the use of phendimetrazine and the concomitant dietary regimen.
- Phendimetrazine may decrease the hypotensive effect of guanethidine.
- The least amount feasible should be prescribed or dispensed at one time in order to minimize the possibility of overdosage.
- The phendimetrazine tartrate pink and yellow tablets contain FD&C yellow No. 5 (tartrazine) which may cause allergic type reactions (including bronchial asthma) in certain susceptible individuals. Although the overall incidence of FD&C yellow No. 5 (tartrazine) sensitivity in the general population is low, it is frequently seen in patients who also have aspirin hypersensitivity.
Adverse Reactions
Clinical Trials Experience
Cardiovascular
=====Central Nervous System=====* Overstimulation, restlessness, insomnia, agitation, flushing, tremor, sweating, dizziness, headache, psychotic state, blurring of vision.
Gastrointestinal
Genitourinary
Postmarketing Experience
There is limited information regarding Postmarketing Experience of Phendimetrazine in the drug label.
Drug Interactions
There is limited information regarding Phendimetrazine Drug Interactions in the drug label.
Use in Specific Populations
Pregnancy
- Safe use in pregnancy has not been established. Until more information is available, phendimetrazine tartrate should not be taken by women who are or who may become pregnant unless, in the opinion of the physician, the potential benefits outweigh the possible hazards.
- Australian Drug Evaluation Committee (ADEC) Pregnancy Category
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Phendimetrazine in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Phendimetrazine during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Phendimetrazine with respect to nursing mothers.
Pediatric Use
Phendimetrazine tartrate is not recommended for use in children under 12 years of age.
Geriatic Use
There is no FDA guidance on the use of Phendimetrazine with respect to geriatric patients.
Gender
There is no FDA guidance on the use of Phendimetrazine with respect to specific gender populations.
Race
There is no FDA guidance on the use of Phendimetrazine with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Phendimetrazine in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Phendimetrazine in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Phendimetrazine in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Phendimetrazine in patients who are immunocompromised.
Administration and Monitoring
Administration
Monitoring
There is limited information regarding Monitoring of Phendimetrazine in the drug label.
IV Compatibility
There is limited information regarding IV Compatibility of Phendimetrazine in the drug label.
Overdosage
- Acute overdosage with phendimetrazine tartrate may manifest itself by the following signs and symptoms: unusual restlessness, confusion, belligerence, hallucinations and panic states. Fatigue and depression usually follow the central stimulation. Cardiovascular effects include arrhythmias, hypertension or hypotension and circulatory collapse. Gastrointestinal symptoms include nausea, vomiting, diarrhea and abdominal cramps. Poisoning may result in convulsions, coma and death.
- The management of overdosage is largely symptomatic. It includes sedation with a barbiturate. If hypertension is marked, the use of a nitrate or rapid-acting alpha receptor-blocking agent should be considered. Experience with hemodialysis or peritoneal dialysis is inadequate to permit recommendations for its use.
DRUG ABUSE AND DEPENDENCE
- Controlled Substance
- Phendimetrazine tartrate tablets are defined by the Drug Enforcement Administration as a Schedule III controlled substance.
Dependence
- Phendimetrazine tartrate is related chemically and pharmacologically to the amphetamines. Amphetamines and related stimulant drugs have been extensively abused and the possibility of abuse of phendimetrazine should be kept in mind when evaluating the desirability of including a drug as part of a weight reduction program. Abuse of amphetamines and related drugs may be associated with intense psychological dependence and severe social dysfunction. There are reports of patients who have increased the dosage to many times that recommended. Abrupt cessation following prolonged high dosage administration results in extreme fatigue and mental depression; changes are also noted on the sleep EEG. Manifestations of chronic intoxication with anorectic drugs include severe dermatoses, marked insomnia, irritability, hyperactivity and personality changes. The most severe manifestation of chronic intoxications is psychosis, often clinically indistinguishable from schizophrenia.
Pharmacology
| |
Phendimetrazine
| |
| Systematic (IUPAC) name | |
| 3,4-dimethyl-2-phenylmorpholine | |
| Identifiers | |
| CAS number | |
| ATC code | none |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox |
| Mol. mass | 191.27 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | Peak plasma levels occur within 1 to 3 hours. Absorption is usually complete by 4 to 6 hours |
| Metabolism | Hepatic |
| Half life | 19-24 hours |
| Excretion | Urinary elimination |
| Therapeutic considerations | |
| Pregnancy cat. |
C (US) |
| Legal status |
C-III (US) |
| Routes | Oral |
Mechanism of Action
- Phendimetrazine tartrate is a phenylalkylamine sympathomimetic amine with pharmacological activity similar to the prototype drugs of this class used in obesity, the amphetamines. Actions include central nervous system stimulation and elevation of blood pressure. Tachyphylaxis and tolerance have been demonstrated with all drugs of this class in which these phenomena have been looked for.
- Drugs of this class used in obesity are commonly known as “anorectics” or “anorexigenics”. It has not been established, however, that the action of such drugs in treating obesity is primarily one of appetite suppression. Other central nervous system actions or metabolic effects, may be involved, for example.
- Adult obese subjects instructed in dietary management and treated with “anorectic” drugs lose more weight on the average than those treated with placebo and diet, as determined in relatively short term clinical trials.
Structure
- Phendimetrazine tartrate, as the dextro isomer, has the chemical name of (2s, 3s,)-3,4-dimethyl-2-phenylmorpholine L-(+)-tartrate (1:1).
- The structural formula is as follows:
This image is provided by the National Library of Medicine.
- Phendimetrazine tartrate is a white, odorless crystalline powder. It is freely soluble in water; sparingly soluble in warm alcohol; insoluble in chloroform, acetone, ether and benzene.
- Each tablet, for oral administration, contains 35 mg of phendimetrazine tartrate.
- Inactive Ingredients: confectioner’s sugar (sucrose and corn starch), lactose monohydrate, povidone, pregelatinized starch, silicon dioxide and stearic acid.
- The pink, white and blue tablets also contain: FD&C blue No. 1 and FD&C red No. 3.
- The pink tablets also contain: FD&C red No. 3 and FD&C yellow No. 5.
- The yellow tablets also contain: FD&C yellow No. 5
Pharmacodynamics
There is limited information regarding Pharmacodynamics of Phendimetrazine in the drug label.
Pharmacokinetics
- The magnitude of increased weight loss of drug-treated patients over placebo-treated patients is only a fraction of a pound a week. The rate of weight loss is greatest in the first weeks of therapy for both drug and placebo subjects and tends to decrease in succeeding weeks. The possible origins of the increased weight loss due to the various drug effects are not established. The amount of weight loss associated with the use of an anorectic drug varies from trial to trial and the increased weight loss appears to be related in part to variables other than the drug prescribed, such as the physician investigator, the population treated and the diet prescribed. Studies do not permit conclusions as to the relative importance of the drug and non-drug factors on weight loss.
- The natural history of obesity is measured in years, whereas the studies cited are restricted to a few weeks duration, thus, the total impact of drug-induced weight loss over that of diet alone must be considered clinically limited.
Nonclinical Toxicology
There is limited information regarding Nonclinical Toxicology of Phendimetrazine in the drug label.
Clinical Studies
There is limited information regarding Clinical Studies of Phendimetrazine in the drug label.
How Supplied
- Phendimetrazine Tartrate Tablets 35 mg are yellow, bisected, round tablet; imprinted "E 76"
- Bottles of 30 - 68788-9743-3
Storage
- Store at 20° to 25°C (68° to 77°F). Protect from moisture.
- Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure, as required.
Images
Drug Images
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Package and Label Display Panel
PHENDIMETRAZINE TARTRATE TABLETS USP, 35 MG LABEL
This image is provided by the National Library of Medicine.
Ingrediensta and Appearance
This image is provided by the National Library of Medicine.
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Patient Counseling Information
There is limited information regarding Patient Counseling Information of Phendimetrazine in the drug label.
Precautions with Alcohol
- Alcohol-Phendimetrazine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
- Bontril®[1]
Look-Alike Drug Names
There is limited information regarding Look alike drug names.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.