pharmacology nervous system presentation

8/7/2019 Pharmacology Nervous System Presentation

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INTRODUCTION

NERVOUSSYSTEM

CNS

BRAIN SOMATIC

NERVOUS

SYSTEM

SPINAL CORD

PARASYMPPATHETIC

NERVOUS SYSTEMSYMPATHETIC

NERVOUS SYSTEM

ANS

PNS

OVERVIEW OF THE ANATOMICAL ORGANIZATION OF THE NERVOUS SYSTEM

Ekman (2002).


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Lemme to the math

what is central nervous system???

It is the most complex of all system inthe body.

It can be stimulated & depressed bydrugs.

To understand the effects of drugs, a basicidea of the important neurotransmittersacting on the CNS & their receptors arevery much essential.

Ekman (2002).


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EXCITATORYTRANSMITTER

INHIBITORYTRANSMITTERS

OTHERTRANSMITTERS

GLUTAMATE

GABA, GLYCINE

NORADRENALINE,DOPAMINE,

5-HT, ACETYLCHOLINE,

HISTAMINE, ADENOSINE

NormallyEkman (2002).


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Udaykumar (2006).


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Udaykumar (2006).


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Udaykumar (2006).


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PSYCHOTHERAPEUTIC AGENTS

1.ANTIPSYCHOTICS/ NEUROLEPTICS /

TRANQUILIZERS AGENT

Udaykumar (2006).


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Psychiatric Illnesses

Pathology :Overactivity of the neurotransmitters

mainly dopamine & probably others

including glutamate (NMDA

receptors) & 5-HT in the brain.

Organics

Mental

Disorder

Psychoses

-schizophrenia

-delusional

(paranoia)

-affective (mood)

disorder

Neuroses

-anxiety

-mood

changes

-panic disorder

Personality

Disorder

-paranoid

-avoidant

-antisocial

Udaykumar (2006).


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CLASS GROUP GENERIC TRADE

Classical / typical

neuroleptics

Phenothiazines

Butyrophenones

CHLORPROMAZINE

HALOPERIDOL

Largactil

Haldol

Atypical

antipsychotics

Clozapine Clozaril, Clozaril,

FazaClo, Clopine,

Clozapine Synthon,Denzapine, Zaponex

1) ANTIPSYCHOTICS

Udaykumar (2006).


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TYPICAL ANTIPSYCHOTICS:

CHLORPROMAZINE (CPZ)

Description:

-White, crystalline solid, practically

insoluble in water & freely soluble in alcohol.

Composition:

-Each mL contains Chlorpromazine hydrochloride 25 mg,

ascorbic acid 2 mg, sodium metabisulfite 1 mg, sodiumsulfite 1 mg and sodium chloride 6 mg in Water for

Injection. pH is 3.4-5.4.

i.McEvoy, K.,Snow, K.,Kester.(2006)

ii. Tatro.S, & Borgsdorf.R. (2006).


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Pharmacodynamic(Mechanism of Action):

-There are 5 subtypes of dopaminereceptors (D1 D5).

-CPZ blocks the action of dopamine(neurotransmitter) through blocking thedopamine D2 receptors in the CNS.

-Dopaminergic overactivitymainly occurat limbic area in which thought to beresponsible for pschizophrenia.




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Udaykumar (2006).


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CHLORPROMAZINE (CPZ)

http://www.dmhweb.dmh.go.th/jvsk/CPSY2/Picture/Chlorpromazine%20100%20mg.jpg


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http://www.dmhweb.dmh.go.th/jvsk/CPSY2/Picture/Chlorpromazine%20100%20mg.jpg


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Pharmacokinetics:

Absorption:

-CPZ is rapidly absorbed from:

a) GIT (rectal)&

b) Parenteral (IM) sites of injection&

c) Oral(PO) administration,

>>the drugs undergoes;

*considerable metabolism duringabsorption (in the GI mucosa) &

*significant first pastthrough the liver;

About 30% bioavailable.




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Distribution:

Highly protein bound (92-97%); Vd is about 21

L/kg. Excreted in breast milk.Elimination:

t of 20-24hrs; Less than 1% is excreted in

the urine.




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Indication & recommended dosage:

1.Psychotic Disorders & Excessive Anxiety,

Tension, & Agitation.

ADULT PEDIATRIC

Inpatient:

PO 25mg tid; increase prn; usually 400

mg/day.IM 25mg initially; may give additional

25 50mg in 1 hr. Increase gradually until

controlled. Up to 2,000mg/day may needed

but generally not for extended periods.

Inpatient:

PO Start low & increase gradually; 50-

100mg/day may be needed in severe casesor 200mg/day or more in older children.

IM

Up to 5 yr of age ; Do not exceed 40mg/day.

5 12 yr of age; Do not exceed 75mg/day if

possible.

Outpatient:

IM 25mg for prompt control; may repeat in

1 hr.

PO 25 50mg tid after regimen. May

initiate oral dosing with 10mg tid or qid or

25 mg bid or tid

Outpatient:

PO 0.5mg/kg q 4 - 6 hr prn;

IM 0.5mg/kg q6-8 hr prn.




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2. Acute Intermittent Porphyria

3.Tetanus

ADULT

PO 25 50mg tid or qid;

IM 25mg tid to qid.

ADULT PEDIATRIC

IM 25 50mg tid to qid

IV 25 50 mg diluted to greater than

or equal to 1mg/mL & administered at

rate of1mg/min

IM/IV 0.5mg/kg q 6 8 hr. When

giving IV, dilute to at least 1mg /L &

administer at rate of1mg/2min.




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4. Nausea & Vomitting

5. During surgery

ADULT PEDIATRIC

PO 1025 mg q 46 hr prn.

PR 100 mg q 6-8 hr prn.

IM 25 mg.

If no hypotension, may give 25 to 50 mg q

4-6hr prn.

PO 0.55mg/kg q 4-6hr.

PR 1.1 mg/kg q 6-8hr prn.

IM 0.55mg/kg q 6-8hr prn.

ADULT

IM 12.5mg; repeat in hr if necessary & if no hypotension.

IV 2mg per fractional injection, at 2-min intervals (max, 25mg)




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6. Presurgical apprehension

7.Intractable hiccoughs/hiccups

ADULT PEDIATRIC

PO 25-50mg 2-3 hr prior to surgery.

IM 12.5-25mg 1-2 hr before surgery.

PO 0.55mg/kg 2-3 hr before surgery.

IM 0.55 mg/kg 1-2 hr before surgery.

ADULT

PO 25-50 mg tid-qid

IM 25-50mg given if symptom persist 2-3days

IV May use slow infusion if hiccoughs persist.




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Contraindication:

-drug allergy-comatose state

-possibly significant CNS depression

-brain damage-liver or kidney disease

-uncontrolled epilepsy




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Warning & precaution

Pregnancy Safety not established

Lactation Excreted in breast milk

Children Do not use in children under 6 mo unless considered

life-saving.

Elderly More susceptible to enhanced effect; consider lower

dose.

Special risk patients Use caution in patients with CV disease.




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Interaction with other medication:

Alcohol & otherCNS depressants May cause increased CNS depression & may

precipitate extrapyramidal reaction.

Anticholinergics Lead to tardive dyskinesia.

Barbiturate anesthetics May increase frequency & severity of

neuromuscular excitation& hypotension.

Beta-blockers Increased plasma levels of beta-blocker &

chlorpromazine.




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Adverse reaction on CNS:

1. Faintness,

2. Drowsiness,

3. Dystonia,

4. Dizziness,

5. Extrapyramidal side effects, EPS

(eg;pseudoparkinsonism, tardive dyskinesia),

6. Muscle spasms,

7. Motor restlessness,

8.

Slurring,9. Insomnia,

10. Vertigo,

11.Seizures,i.McEvoy, K.,Snow, K.,Kester.(2006)



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Overdosage: Signs & symptoms

1. CNS depression

2. Hypotension

3. Extrapyramidal symptoms4. Hypothermia

5. Hyperthermia

6. Coma

7. Cardiac Arrhythmias




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Storage condition:

-Protect from light.

-Store at 20-25C (68-77F), excursions

permitted to 15-30C (59-86F).

-Protect from freezing.

Manufecturer:

Baxter Deerfield,

IL 60015 USA.

462-324-00




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ATYPICAL ANTIPSYCHOTIC :

CLOZAPINE


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Drug: Clozapine

Strength(s): 100 mg

Color: Green

Shape: Round

Description:

Drug: Clozapine

Strength(s): 25 mg

Color: Peach

Shape: Round

Drug: Clozapine

Strength(s): 200 mg

Color: Yellow

Shape: Elliptical / Oval

Drug: Clozapine

Strength(s): 50 mg

Color: Yellow

Shape: Round

http://www.drugs.com/imprints.php?action=search&drugname=clozapine


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Composition:

i. colloidal silicon dioxide,ii. crospovidone,

iii. lactose monohydrate,

iv. magnesium stearate,

v. microcrystalline cellulose,vi. sodium lauryl sulfate.

*25 mg tablet contains FD&C Red No. 40 Aluminum Lake.

*100 mg tablet contains FD&C Blue No.2Aluminum Lake.




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pharmacology nervous system presentation

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