Pharmacy Practice Lectures for Pharm-D Students

1. PATIENT PROFILE & PATIENT COUNSELING
C. DRUG PROFILE OF ATLEAST 25
IMPORTANT MEDICATIONS
BENZODIAZEPINES
CLINICAL PHARMACY
BY
Zul Kamal
DEPARTMENT OF PHARMACY
SHAHEED BENAZIR BHUTTO UNIVERSITY, SHERINGAL

2. BENZODIAZEPINES
Benzodiazepines are the most widely used anxiolytic drugs.
They have largely replaced barbiturates and meprobamate in the
treatment of anxiety, because the benzodiazepines are safer and more
effective

3. PHARMACOKINETICS
 ADMINISTERATION
• Orally
• Parentrally
 ABSORPTION
• It is highly lipid soluble weak basic compounds so absorption is from
Duodenum.
• It is either completely absorbed as such OR it may undergo acid
hydrolysis; e.g.
Clorazepam converts to Dismethyldiazepam then absorbed in blood
circulation.
 DISTRIBUTION
• All body tissues
• 60-95% Protein bound
 METABOLISM
Liver
 EXCRETION
through Urine

4. PHARMACODYNAMIC
MECHANISM OF ACTION
 Target for the Benzodiazepine actions are GABA-
Receptors.
 These GABA-Receptor causes opening of Chloride
Channels which causes Hyperpolraization of the cell
which blocks the repetitive action potential.

7. INDICATIONS
Reduction of anxiety
• At low doses, the benzodiazepines are anxiolytic.
They are thought to reduce anxiety by selectively
enhancing GABAergic transmission in neurons.
Sedative and hypnotic actions
All of the benzodiazepines used to treat anxiety
have some sedative properties, and some can
produce hypnosis (artificially produced sleep) at
higher doses.

8. Muscle disorders
• At high doses, the benzodiazepines relax the
spasticity (neurological disorders) of skeletal
muscle, probably by increasing presynaptic
inhibition in the spinal cord, where the GABAA
receptors are largely located.
• Baclofen is a muscle relaxant that is believed to
affect GABAb receptors at the level of the spinal
cord.
• Example: Multiple Sclerosis (Chronic, unpredictable, and
often progressive disease of the central nervous system that attacks
and destroys tissues in the brain and spinal cord)

9. Cerebral Palsy
A disorder or movement or posture as a result of non-
progressive but permanent damage to the developing
brain.
Epilepsy
• Clonazepam is used for long term use of epilepsy
• Diazepam (status epilepticus)
Pre-anesthetic Medications
It causes amnesia (memory loss) and muscle relaxation
Insomnia
• Florazepam is used for those people who has difficulty in
onset of sleep)

10. CONTRAINDICATIONS
 Lactation (secretes in breast milk).
 Chronic Obstructive Pulmonary Disease.
 Glaucoma

11. ADVERSE EFFECTS
 Ataxia, Headache, Vertigos, Blurred Vision and
Weakness.
 In hypnotic doses it causes motor in-cordination of
muscles.
 Dry mouth, bitter taste and hallucination
 Restlessness
 Euphoria
 Hypnopompic behavior (Occurs when a person is neither
full in sleep nor full awakened)

12. DOSE ,DOSAGE FORM AND BRAND NAME
 DOSAGE FORM
• Tablets
• Injectables
 BRAND NAME:
Diazepam 2-10 mg BID
Valium (Roche), Tab 5, 10 mg, Inj 10 mg
Relaxe (Wilshire), Tab 5 mg,
Alprazolam 0.25-0.5 mg TID
Xanax (Park Davis), Tab 0.25, 0.5 mg
Hilazin (Himont), Tab 0.25, 0.5 mg
Bromazepam 3-18 mg/day BID or TID
Laxillium (Sami), Tab 3 mg
Relaxin (Mactor), Tab 3 mg
Lorazepam 1-4 mg/Day
Ativan (Wyeth), Tab 1, 2 mg