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Drug Administration Laboratory of Pharmacology Department of Pharmacology and Therapeutics Faculty of Medicine Diponegoro University 2012

Drug administration and pharmacology of phenobarbital

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laboratory work for drug administration in pharmacology class. Diponegoro University, School of Medicine

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Page 1: Drug administration and pharmacology of phenobarbital

Drug Administration

Laboratory of PharmacologyDepartment of Pharmacology and Therapeutics

Faculty of Medicine Diponegoro University2012

Page 2: Drug administration and pharmacology of phenobarbital

• Enteral (oral? Intubation= nasogastric tube?)

• Parenteral (Injection= Intramuscular/Intravenous/Intraperitoneal/Subcutan)

• Inhalation• Topical

Page 3: Drug administration and pharmacology of phenobarbital

Drug Administration

• oral• sublingual• Rectal/rectal suppository• application to other epithelial surfaces (e.g. skin, cornea, vagina

and nasal mucosa) topical-vaginal suppository• inhalation• Injection

– Subcutaneous– Intramuscular– Intravenous– Intrathecal– intravitreal.

Page 4: Drug administration and pharmacology of phenobarbital
Page 5: Drug administration and pharmacology of phenobarbital

Enteral Administration

Page 6: Drug administration and pharmacology of phenobarbital

Phenobarbital

• Barbiturate drug, trade name Luminal

• Mainly as Anticonvulsant• Hypnotic effect, Sedative effect,• Bioavailability after proper

administration = 95%• Metabolism= Hepatic

(Cytochrome P450)• Half-life= 53-118 hours• Excretion= Renal and Fecal

Page 7: Drug administration and pharmacology of phenobarbital

Clinical Use

• Phenobarbital is useful in the treatment of partial seizures and generalized tonic-clonic seizures, although the drug is often tried for virtually every seizure type, especially when attacks are difficult to control

• Depresses neurons activities via Reticular Formation, Induces sleep (Sedative, Hypnotics, and Anesthetics)

Page 8: Drug administration and pharmacology of phenobarbital

Formantio Reticularis

Page 9: Drug administration and pharmacology of phenobarbital

GABA-mediated chloride ion channel

from Zorumski CF, Isenberg KE: Insights into the structure and function of GABA receptors: Ion channels and psychiatry. Am J Psychiatry 1991;148:162.)

Page 10: Drug administration and pharmacology of phenobarbital

Pharmacokinetics

• The rates of oral absorption of sedative-hypnotics differ depending on a number of factors, including lipophilicity.

• Most of the barbiturates and other older sedative-hypnotics, as well as the newer hypnotics (eszopiclone, zaleplon, zolpidem), are absorbed rapidly into the blood following oral administration.

Page 11: Drug administration and pharmacology of phenobarbital

Pharmacodynamics• Benzodiazepines and phenobarbital augment

the activation of the GABAA receptor by physiologically released amounts of GABA.• Elongates the GABA-mediated Chloride Ion

Channel Opening.• Elongates GABA and Glycine Inhibitory Effect • Chloride influx is increased, counteracting

depolarization. • Depresses the CNS via Reticular Formation.• Induces sleep (Sedative, Hypnotics, and

Anesthetics)