Phentermine



Phentermine
Systematic (IUPAC) name
2-methyl-1-phenylpropan-2-amine and 2-methyl-amphetamine
Identifiers
CAS number 122-09-8
ATC code C01CA11
PubChem 4771
DrugBank APRD00093
Chemical data
N 
Mol. mass 149.233 g/mol
Pharmacokinetic data
Bioavailability Peak plasma levels occur within 1 to 4.5 hours. Absorption is usually complete by 4 to 6 hours
Protein binding Approximately 96.3%
Metabolism hepatic
Half life 16 to 31 hours
Excretion Urinary elimination
Therapeutic considerations
Pregnancy cat.

C(United States); ? (Australia)

Legal status

C-IV (US)

Routes Oral

Phentermine is an appetite suppressant of the phenethylamine class.

It is approved as an appetite suppressant to help reduce weight in obese patients when used short-term and combined with exercise, diet, and behavioral modification. It is typically prescribed for individuals who are at increased medical risk because of their weight and works by helping to release certain chemicals in the brain that control appetite.

Commercial trade names

  • Adipex P (Immediate release)
  • Anoxine-AM®
  • Fastin® (discontinued)
  • Ionamin® (Slow Release Resin, Australia, discontinued in the US)
  • Duromine® (Slow Release Resin, New Zealand)
  • Obephen®
  • Obermine®
  • Obestin-30®
  • Phentrol®
  • Phenterex®
  • Phentromin®
  • Pro-Fast SA
  • Redusa
  • Panbesy
  • Phentermine Trenker
  • Obenix
  • Oby-Trim

History

In 1959 phentermine first received approval from the FDA as an appetite suppressing drug. Phentermine hydrochloride then became available in the early 1970s. It was previously sold as Fastin® from King Pharmaceuticals for Fen-Phen.

A study was published in 1992 that Fen-Phen was more effective than diet and exercise with few side effects. However, in 1997 after 24 cases of heart valve disease in Fen-Phen users, fenfluramine and dexfenfluramine were voluntarily taken off the market at the request of the FDA. Studies later proved that nearly 30% of people taking fenfluramine or dexfenfluramine had abnormal valve findings. The FDA did not ask manufacturers to remove phentermine from the market.

Phentermine is still available by itself in most countries, including the U.S. However, because it is similar to Convention on Psychotropic Substances.[1] In the United States, it is classified as a Schedule IV controlled substance under the Controlled Substances Act.

Mechanism of action

  Phentermine, like many other prescription drugs, works with phendimetrazine. The neurotransmitters signal a fight-or-flight response in the body which, in turn, puts a halt to the hunger signal. As a result, it causes a loss in appetite because the brain does not receive the hunger message.

Dosing and administration

Generally, it is recommended by the drug tolerance, whereby phentermine loses its appetite-suppressing effects after the body adjusts to the drug. On the contrary, it has been shown that phentermine did not lose effectiveness in a 36-week trial.[2] Due to the risk of insomnia, it is generally recommended that the drug be taken either before breakfast or 1-2 hours after breakfast.

Contraindications and warnings

  • Patients with the following should not use Phentermine:
    • An allergy to any ingredient in Phentermine or other pseudoephedrine)
    • Are also taking monoamine oxidase inhibitor (MAOI) (eg, phenelzine) in the last 14 days
    • Have severe high blood pressure, an overactive thyroid, glaucoma, heart or blood vessel disease, or severe narrowing of the blood vessels
    • Are in an agitated state, or have a history of substance abuse
  • Some medical conditions may interact with Phentermine, patients with the following should consult with their doctor before using phentermine:
    • Are pregnant, planning to become pregnant, or are breast-feeding
    • Are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
    • Have allergies to medicines, foods, or other substances
    • Have a brain or spinal cord disorder, hardening of the arteries, high blood pressure, high cholesterol or lipid levels
  • Some medicines may interact with Phentermine, such as the following:
    • Dexfenfluramine, fenfluramine, furazolidone, or MAOIs (eg, phenelzine) because the risk of serious side effects, such as increasing headache, high blood pressure, slow heart rate, elevated temperature, or possibly fatal lung problems, may be increased
    • Serotonin specific reuptake inhibitors (eg, fluoxetine) because the risk of their side effects may be increased by Phentermine
    • Guanadrel or guanethidine because their effectiveness may be decreased by Phentermine

Side effects

Generally, phentermine appears to be relatively well tolerated.[3] It can produce side effects consistent with its catecholamine-releasing properties, e.g., tachycardia (increased heart rate) and elevated blood pressure, but the incidence and magnitude of these appear to be less than with the amphetamines. Because phentermine acts through sympathomimetic pathways, the drug may increase blood pressure and heart rate. It may also cause palpitations, restlessness, and insomnia. Additionally, phentermine has the potential to cause physical and psychological dependence.

More Common Symptoms

  • Insomnia
  • Increased blood pressure
  • Irritability
  • Nervousness
  • Sense of well-being

Less Common to Rare Symptoms

  • Blurred vision
  • Change in sexual desire
  • Clumsiness
  • Confusion
  • Diarrhea
  • Dizziness
  • Dry mouth
  • Headache
  • Irregular heartbeat
  • Nausea or vomiting
  • Psychosis
  • Skin rash or itching
  • Stomach pain
  • Tiredness
  • Unpleasant taste

Possible Overdose Symptoms

  • Confusion
  • Convulsions (seizures)
  • Dizziness
  • Fast Breathing
  • Fever
  • Hallucinations
  • Hostility with urge to attack
  • Irregular blood pressure
  • Irregular heartbeat
  • Lightheadedness or Fainting
  • Mental Depression, following a period of excitement
  • Tremors, Trembling, or Shaking
  • Overactive Reflexes
  • Panic
  • Restlessness
  • Severe nausea, vomiting or diarrhea
  • Stomach cramps
  • Tiredness or Weakness


References

  1. ^ Incb.org (PDF file)
  2. ^ PMID 11054601
  3. ^ Nelson DL, Gehlert DR. (2006). Central nervous system biogenic amine targets for control of appetite and energy expenditure. (HTML). Endocrine. 2006 Feb;29(1):49-60. PubMed. Retrieved on 6 May, 2006.


 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Phentermine". A list of authors is available in Wikipedia.