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King Saud University College Of Pharmacy Department of Pharmacology. CNS Depressant Drugs. 322 PHL Lab # 4. Classification of CNS Depressant Drugs According to Their Pharmacological action. 1- Sedative – hypnotics 2- Tranquillizers 3- Anesthetics . General signs for CNS depressants.
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King Saud UniversityCollege Of PharmacyDepartment of Pharmacology CNS Depressant Drugs 322PHL Lab # 4
Classification of CNS Depressant Drugs According to Their Pharmacological action 1- Sedative – hypnotics 2- Tranquillizers 3- Anesthetics
General signs for CNS depressants 1- ↓ vitality 2- ↓ excitability 3- ↓ HR & RR
I. Sedative – hypnotics Sedatives: Drugs which calm the patient & cause sedation and in large doses they induce sleeping. Hypnotics: Drugs which induce sleep that resembles to the natural sleep e.g. Barbiturates
Natural Sleep Sleep: Physiological depression of consciousness. Sleep cycle: Starts with latency period → NREM → REM → cycles of NREM alternate with REM (about 4 cycles)
II- Tranquillizers Definition: Tranquillizers are drugs which relief mental anxiety & stress without affecting the consciousness. e.g. Chlorpromazine (CPZ) MOA: It is D2 , 5-HT , H1, α1 antagonist
III- Anesthetics Definition: Drugs which cause unconsciousness & generalized loss of pain sensation, thus allow surgical procedures to be carried out . e.g. thiopental (IV) , halothane (inhalation) MOA: Interfering with propagation of nerve impulses by interfering with electrolytes conductance through the cell membrane.
1- Barbiturates MOA: • They have GABA like action • (They facilitating the GABA action → mediate opening ofchloride channels →increase CL influx →hyperpolarization Classification according to their duration of action: 1-Long-acting . 2-Intermediate-acting . 3-Short acting . 4-Ultrashort acting .
2- Benzodiazepines • Benzodiazepines enhance the response to GABAa by facilitating the opening of GABA-activated chloride channels
2- Benzodiazepines • They bind specifically to a regulatory site of the receptor, distinct from the GABA-binding site, and act allosterically to increase the affinity of GABA for the receptor e.g. Diazepam (sedative) (Triazolam(hypnotic
3- Non-barbiturate Non-BZD • (5-HTA1) agonist e.g. buspirone. • Chloral hydrate (prodrug) converted to trichloroethanol. • Antihistamine e.g. diphenhydramine. • Paraldehyde . • Promethazine .
Specific signs of sedative-hypnotic Drugs: Thiopental, Phenobarbital & chloral hydrate . Signs: 1- Staggering gait . 2- Sleeping posture . 3- Loss of righting reflex (onset time) . 4- ↓ Touch & pain reflexes ( lostwith thiopental ) .
Specific signs for CBZ Signs: 1- No loss of righting reflex . 2- Creeping gait. 3- Abdomen touches the ground. 4- State of catalepsy (loss of muscles control)→(onset time) 5- ↓ Touch & pain reflexes.