pharmacology nervous system presentation
TRANSCRIPT
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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
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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
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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
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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.
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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.
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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.
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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.
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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.
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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)
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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.
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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Contraindication:
-drug allergy-comatose state
-possibly significant CNS depression
-brain damage-liver or kidney disease
-uncontrolled epilepsy
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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.
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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.
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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)
ii. Tatro.S, & Borgsdorf.R. (2006).
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Overdosage: Signs & symptoms
1. CNS depression
2. Hypotension
3. Extrapyramidal symptoms4. Hypothermia
5. Hyperthermia
6. Coma
7. Cardiac Arrhythmias
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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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.
i.McEvoy, K.,Snow, K.,Kester.(2006)
ii. Tatro.S, & Borgsdorf.R. (2006).
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