DRUG
PROFILE
Drug:
(Prazepam)
Submitted to: Dr Saira
Submitted by: Anoosha Aslam
Prazepam is a benzodiazepine derivative drug
developed by Warner-Lambert in the 1960s. It
possesses different properties:
anxiolytic
Anticonvulsant
sedative
skeletal muscle relaxant.
Prazepam is a prodrug for desmethyldiazepam
which is responsible for the therapeutic effects of
prazepam.
PRODUCT DESCRIPTION
BRAND DOSAGE STRENHT PACK ROU MANUFACT
NAME FORM SIZE TE URER
Centrax Oral 3mg 30 or 50 Oral Cenexi
tablets 6mg tabs per
pack
Demetri Oral 25mg 10,20,30 Oral MS DORMAN
n tablets or Tabs per
capsules pack
Prazene Oral 1mg 10,20,30 Oral Abbott
tablets 2mg Tabs per laboratries
5mg pack
Trepidan Oral 4mg 10 tabs Oral MS DORMAN
tablets 8mg 30 tabs
lysanxia Oral 10mg 20 tabs Oral Roche
tablets 20mg
CHEMISTRY OF THE DRUG
1: Molecular Formula
PHYSICAL
C18H14Cl2N2O
PROPERTIES:
2: Molecular Weight
343.23 g/mol
3: Appearance
white to off-white crystalline powder.
4: Solubility
slightly soluble in water.
It is more soluble in organic solvents like ethanol, methanol, and
chloroform.
5: Melting Point
The melting point of prazepam is approximately 147–150°C.
6: Boiling Point
300°C
7: pKa (Acidity Constant)
7.9 which suggests that it is a weak acid in solution.
8: Stability
Prazepam is stable under normal storage conditions, which typically
involve keeping it in a cool, dry place and away from light.
PHARMACOKINETICS
Absorption: Well absorbed in GIT.
Volume of Distribution: widely distributed
throughout the body including CNS (cross BBB)
.
Plasma Protein binding: 90%
Metabolism:extensive hepatic metablism by
CYP450 enzyme system particularly CYP3A4
Half life: 30 to 100 hrs
Excretion: renal excretion
Onset of action: 30 mins to 1hr after oral
administration
Shelf life: 2 to 3 years
CLINICAL PHARMACOLOGY
Drug class: GABA stimulator
Pharmaological class: benzodiazepine
Mechanism of action:
Prazepam is believed to stimulate GABA receptors in the
ascending reticular activating system. Since GABA is
inhibitory receptor stimulation increases inhibition,
calcium influx increases, hyperpolarization increases and
blocks both cortical and limbic arousal following
stimulation of the brain stem reticular formation.
Indications:
For the treatment of:
Generalized Anxiety Disorder (GAD)
Acute Anxiety or Short-Term Anxiety Episodes
Anxiety-related Sleep Disturbances
Muscle relaxant Acute stress
Sedative reactions
Contraindications
Hypersensitivity to Prazepam:
• Prazepam should not be used in individuals who are allergic
to the drug or to other benzodiazepines, as this can cause
severe allergic reactions.
Acute Narrow-Angle Glaucoma:
• prazepam can worsen intraocular pressure, potentially
leading to an acute angle-closure glaucoma episodes.
Severe Respiratory Insufficiency:
• Since prazepam has sedative properties that can depress
the respiratory system, it should not be used in individuals
with severe respiratory failure,
• such as in cases of severe chronic obstructive pulmonary
disease (COPD) or sleep apnea.
Severe Hepatic Insufficiency.
Myasthenia Gravis:
• a condition characterized by weakened muscles. The muscle-
relaxant effects of prazepam may exacerbate muscle weakness
and worsen the condition.
Pregnancy (especially. during the first trimester).
Breastfeeding mothers.
Recommended Dosage
Recommended route: Oral
Recommended dose:
• Initial Adult Dose
:Anxiety:starting dose is 10 mg once a day.
• Maintenance Dose:
Ranges from 10 mg to 20 mg per day, depending on how well the
patient responds to the medication. This dose is typically divided into
1-2 dose per day.
• Maximum Dose:
30 mg per day, divided into 2-3 doses.
• Elderly Patients or Patients with Hepatic Impairment:
In older adults or those with liver problems, a lower dose may be
recommended (e.g., 5 mg to 10 mg per day) due to decreased
metabolism and increased sensitivity to benzodiazepines.
• Tapering and Discontinuation:
If prazepam has been used long-term and discontinuation is necessary,
the dose should be gradually reduced under the supervision of a
healthcare provider to avoid withdrawal symptoms.
Side Effects
o Drowsiness or sedation (common due to its calming
effect)
o Dizziness or lightheadedness
o Fatigue or feeling unusually tired
o Impaired coordination or muscle weakness
o Memory problems (such as difficulty recalling recent
events)Headache
o Dry mouth
o Nausea or mild gastrointestinal discomfort
o Blurred vision
Storage precautions
• Store at room temperature (20°C to 25°C or 68°F to 77°F).
• Keep away from heat, moisture, and light.
• Store in a secure place, out of reach of children.
• Keep in the original container and check expiration dates.
• Dispose of the medication safely.
Antidote
The primary antidote for benzodiazepine overdose, including
prazepam, is flumazenil.
Flumazenil as an Antidote for Prazepam Toxicity:
Mechanism of Action:
Flumazenil is a benzodiazepine receptor antagonist that
works by reversing the effects of benzodiazepines like
prazepam at the GABA-A receptors in the brain. It
competitively binds to the same receptor sites that
benzodiazepines affect, effectively reversing sedation,
respiratory depression, and other CNS depressant effects.
Toxicology
• Sedation and somnolence (severe drowsiness)
• Dizziness or lightheadedness
• Ataxia (lack of muscle coordination)
• Hypotension (low blood pressure)
• Respiratory depression (slow, shallow breathing)
• Confusion or disorientation
• Coma (in severe cases)
• Bradycardia (slow heart rate)
• Hypothermia (low body temperature)
• Slurred speech
• Weakness or muscle hypotonia (decreased muscle tone)
References:
LIPPINCOTT PHARMACOLOGY
CHAT GPT
KATZUNG AND TREVERS
PHARMACOLOGY
