Medopam

Medopam Uses, Dosage, Side Effects, Food Interaction and all others data.

Medopam is a short-acting benzodiazepine. It increases neuronal membrane permeability to Cl ions by binding to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron w/in the CNS (including the limbic system, reticular formation) and enhancing the GABA inhibitory effects resulting in hyperpolarisation and stabilisation.

Benzodiazepines, including oxazepam, exert their sedative and anxiolytic effects by potentiating the effects of endogenous GABA, the primary inhibitory neurotransmitter in the CNS. Compared to other benzodiazepines, it has relatively low potency and a moderate duration of action. Medopam should be administered with caution to patients for whom a drop in blood pressure may lead to cardiac complications as, in rare cases, it may cause hypotension.

Trade Name Medopam
Availability Prescription only
Generic Oxazepam
Oxazepam Other Names (RS)-Oxazepam, Oxazepam
Related Drugs escitalopram, alprazolam, duloxetine, Lexapro, Xanax, diazepam, atenolol, Cymbalta, Valium, Tenormin
Type
Formula C15H11ClN2O2
Weight Average: 286.713
Monoisotopic: 286.050905313
Protein binding

Plasma protein binding is approximately 89%, likely to albumin.

Groups Approved
Therapeutic Class Benzodiazepine hypnotics, Benzodiazepine sedatives
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Medopam
Medopam

Uses

Medopam is used in the treatment of anxiety disorders, including anxiety associated with depression. This drug seems to be particularly effective for anxiety, tension, agitation and irritability in older people. It is also prescribed to relieve symptoms of acute alcohol withdrawal.

Medopam is also used to associated treatment for these conditions: Alcohol Withdrawal Syndrome, Anxiety, Anxiety Disorders

How Medopam works

Like other benzodiazepines, oxazepam exerts its anxiolytic effects by potentiating the effect of gamma-aminobutyric acid (GABA) on GABA(A) receptors, the main inhibitory neurotransmitter receptors in the mammalian brain. GABA(A) receptors are a component of GABA-gated ionotropic chloride channels that produce inhibitory postsynaptic potentials - following activation by GABA, the channel undergoes a conformational change that allows the passage of chloride ions through the channel. The inhibitory potentials produced by GABA neurotransmission play an integral role in the suppression and control of epileptiform nerve firing such as that seen in epilepsy, which makes the GABA system a desirable target in the treatment of epilepsy.

Benzodiazepines are positive allosteric modulators of GABA(A) function. They bind to the interface between alpha (α) and gamma (γ) subunits on the receptor, commonly referred to as the benzodiazepine binding site, and modulate the receptor such that its inhibitory response to GABA binding is dramatically increased.

Dosage

Medopam dosage

Adult:

  • Mild to Moderate Anxiety with Tension, Irritability and Agitation: The usual dose is 10 to 15 mg 3 or 4 times per day.
  • Severe Anxiety, Depression with Anxiety, or Alcohol Withdrawal: The usual dose is 15 to 30 mg, 3 or 4 times per day.

Children: Safety and effectiveness have not been established for children less than 6 years of age, nor have dosage guidelines been established for children 6 to 12 years. Doctor will adjust the dosage to fit the child's needs.

Older adults: The usual starting dose is 10 mg, 3 times a day. Doctor may increase the dose to 15 mg 3 or 4 times a day, if needed.

Renal Impairment: No dosage adjustment needed.

Side Effects

Side effects cannot be anticipated. If any develop or change in intensity, doctor should be informed immediately. Doctor will determine if it is safe for a patient to continue taking Medopam. More common side effect includes drowsiness. Less common or rare side effects include: Blood disorders, change in libido, dizziness, excitement, fainting, headache, liver problems, loss or lack of muscle control, nausea, skin rashes or eruptions, sluggishness or unresponsiveness, slurred speech, swelling due to fluid retention, tremors, vertigo, yellowed eyes and skin. Side effects due to rapid decrease or abrupt withdrawal from Medopam: Abdominal and muscle cramps, convulsions, depressed mood, inability to fall or stay asleep, sweating, tremors, vomiting.

Toxicity

The oral LD50 in rats and mice is >8000 mg/kg and 1540 mg/kg, respectively.

Symptoms of oxazepam overdose are likely to be consistent with its adverse effect profile and range from mild to severe, sometimes fatal, CNS depression. Treatment should include gastric decontamination, via lavage or induced vomiting, followed by symptomatic and supportive measures. The benzodiazepine antagonist flumazenil may be used in hospitalized patients as an adjunct to non-pharmacological management, but may increase the risk of seizure in long-term benzodiazepine users and in cyclic antidepressant overdose.

Precaution

This drug may make dizzy, drowsy or cause blurred vision; caution should be taken while engaging in activities requiring alertness such as driving or using machinery. Limit should be maintained while taking alcoholic beverages. Caution is advised when using this drug in the elderly because they may be more sensitive to the effects of the drug, especially the drowsiness effect.

Interaction

Medopam may intensify the effects of alcohol. It may be best to avoid alcohol while taking this medication. If Medopam is taken with certain other drugs, the effects of either could be increased, decreased, or altered. It is especially important to check with a doctor before combining Medopam with the following:

  • Antihistamines such as Diphenhydramine
  • Narcotic painkillers such as Oxycodone and Pethidine
  • Sedatives such as Secobarbital and Triazolam
  • Tranquilizers such as Diazepam and Alprazolam

Food Interaction

  • Avoid alcohol. Co-administration with alcohol may potentiate the CNS effects of oxazepam.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Elimination Route

Following oral administration, peak plasma levels (Cmax) averaged 450 mg/mL and occurred approximately 3 hours (Tmax) after dosing.

Half Life

The mean elimination half-life of oxazepam is 8.2 hours.

Elimination Route

Medopam is primarily eliminated in the urine as its glucuronide metabolite, with the feces containing approximately 21% of the unchanged drug. The majority of an orally ingested dose of oxazepam is excreted within 48 hours.

Pregnancy & Breastfeeding use

This medication is not recommended for use during pregnancy due to the potential possible fetal harm. Based on information from related drugs, this drug may pass into breast milk and may have undesirable effects on a nursing infant. Therefore, breast-feeding while using this medication is not recommended.

Contraindication

The drug is contraindicated in individuals who have an allergic reaction to Medopam or other benzodiazepines such as diazepam. Medopam should not be prescribed if any patient is being treated for mental disorders which are more serious than anxiety.

Acute Overdose

An overdose of Medopam can be fatal. Symptoms of mild Medopam overdose may include: Confusion, drowsiness, lethargy. Symptoms of more serious overdose may include: Coma, hypnotic state, lack of coordination, limp muscles and low blood pressure.

Storage Condition

Store in a cool and dry place, protected from light and moisture. Keep out of reach of children.

Innovators Monograph

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*** Taking medicines without doctor's advice can cause long-term problems.
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