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Psychopharmacology
Psychopharmacology
Introduction
• Psychopharmacology is the study of the regulation and stabilization of
emotions, behavior, and cognition through the interactions of
neurotransmitters and drugs
• These drugs are referred to as psychotropic agents or psychoactive or
psychotherapeutic drugs.
Classification of psychotropic drugs
1. Antipsychotic agents
2. Antianxiety agents (anxiolytics) and hypnotics
3. Antidepressants
4. Antimanic agents
5. Anticonvulsants
6. Anticholinergic or antiparkinsonism agents, which are used to alleviate extrapyramidal
symptoms or adverse effects of psychotropic agents
The science of psychopharmacology
• The science of psychopharmacology focuses on neurotransmission.
• Neurotransmitters undergo six steps, each of which offers a potential target for therapeutic
intervention by a drug;
1. Synthesis
2. Vesicular uptake
3. Transmitter release
4. Receptor binding
5. Cellular re-uptake
6. Transmitter metabolism.
Antipsychotic Medication
• Antipsychotic drugs are also called major tranquillizers or neuroleptics.
• Antipsychotic drugs are derived from several chemical groups and broadly categorized as;
1. Typical or traditional phenothiazines
2. Atypical newer drugs.
Mode of action
• They occupy or block dopamine receptors in the brain thereby decreasing the effects of
dopamine.
• Antipsychotic effects occur when the drug has been given for a few weeks.
Indications
• Treatment of schizophrenia and other psychotic disorders.
• Selected agents are used in the treatment of bipolar mania
• Others uses include;
Antiemetics (chlorpromazine, perphenazine, promethazine)
Treatment of intractable hiccoughs (chlorpromazine)
Control of tics and vocal utterances in Tourette’s disorder (haloperidol, pimozide).
Antipsychotic Medication
• Manifestations of hyperarousal e.g. anxiety, agitation, hyperactivity, insomnia, aggressive
or combative behaviour are relieved more quickly than hallucinations, delusions and
thought disorders.
• These agents also have antiemetic properties.
• Drugs should be given using the following time frame:
Six months for first psychotic episode.
One year period for second psychotic episode.
Indefinite period for third and later psychotic episodes.
Categories of antipsychotic drugs
1. Phenothiazines
2. Butyrophenones
3. Thioxanthenes
4. Phenothiazine like
5. Atypical
1. Phenothiazines
Generic Name Trade Name Daily Dose Range
Chlorpromazine Largactil 300-1000mgs
Thioridazine Melleril 50-800mg
Acetophenazine Tindal 80-120mg
Mesoridazine serentil 100-400mg
Promazine sprine 10-200mg
Fluphenazine Moditen 2.5-20mg
Trifluoperazine Stelazine 5-30mg
2. Butyrophenones
Generic Name Trade Name Daily Dose Range
Haloperidol Haldol, Serenace 1-20mg
3. Thioxanthenes
Thiothixene Navane 6-60mgs
Flupenthixol Depixol 6-18mg
Zuclopenthixol Clopixol 20-150mg
2. Phenothiazine like
Generic Name Trade Name Daily Dose Range
Sulpride Domatil,Sulparex 200-2400mg
Molindone Lidone 50-400mgs
Loxapine Loxitane 60-250mgs
Pimozide Orap 2-10mg
5. Atypical
Generic Name Trade Name Daily Dose Range
Clozapine clozaril 50-900mg
olanzapine zyprexa 5-10mg
Quetiapine Seroquel 25-50mg
Risperodone Risperdal 2-8mg
6. Deport injections
Generic Name Trade Name Daily Dose Range Group
Fluphenazine
decanoate
Modecate 12.5-100mg(IM 2
Weekly)
Phenothiazines
Zuclopenthixol
Acetate
Clopixol
Acuphase
50-150mg every
2-3 days
Thioxanthenes
Haloperidol
decanoate
Haldol
decanoate
50-300mg (IM 4
weekly)
Butyrophenon
Contraindications/Precautions
Typical antipsychotics are contraindicated in:
 Clients with known hypersensitivity (cross-sensitivity may exist among phenothiazines).
 Patients in comatose states or when central nervous system (CNS) depression is evident
 Blood dyscrasias
 Clients with Parkinson’s disease
 Narrow angle glaucoma
 Liver, renal, or cardiac insufficiency; or those with poorly controlled seizure disorders
Side Effects
• The effects of these medications are related to blockage of a number of receptors for which
they exhibit various degrees of affinity.
• Dopamine blockage results in extrapyramidal symptoms (EPS) and prolactin elevation
(galactorrhea; gynecomastia).
• Cholinergic blockade causes anticholinergic side effects (dry mouth, blurred vision,
constipation, urinary retention and tachycardia).
• Blockage of the alpha1-adrenergic receptors produces dizziness, orthostatic hypotension,
tremors, and reflex tachycardia.
Side Effects
• Histamine blockade is associated with weight gain and sedation.
• Skin reactions such as urticaria, dermatitis, and pigmentation of the skin
• Photosensitivity
• Gastrointestinal distress such as nausea, heartburn, and jaundice
• Decreased libido, retrograde ejaculation, and gynecomastia (men)
• Amenorrhea
Extrapyramidal side effects
• The extrapyramidal system is a biological neural network that is part of the motor system
causing involuntary actions.
• The system is called extrapyramidal to distinguish it from the tracts of the motor cortex that
reach their targets by traveling through the pyramids of the medulla
• Antipsychotic medications commonly produce extrapyramidal symptoms as side effects,
especially typical ones.
• Extrapyramidal symptoms are caused by dopamine blockade or depletion in the basal
ganglia; this lack of dopamine often mimics idiopathic pathologies of the extrapyramidal
system.
Functions of extrapyramidal tract
• Control the movement of the eye balls
• Control of tone, posture and equilibrium
• Control of complex movements of the body and limbs e.g. coordinated movement of
arms and legs during walking
• Exert tonic inhibition control over the lower centres
Extrapyramidal side effects
Side Effect Symptoms Onset and prevalence
Parkinsonism Motor retardation or akinesia,
characterized by masklike appearance,
rigidity, tremors, pill rolling, excessive
salivation(sialorrhea)
Generally occurs after first
week of treatment or
before second month
Akathisia (motor
restlessness)
Constant state of movement,
characterized by restlessness, difficulty
sitting still, or strong urge to move
about
Generally occurs 2 weeks
after treatment begins
Acute dystonic
reactions (disturbance
of movement involving
the muscles of the
head, neck, trunk, or
limbs)
Irregular, involuntary spastic muscle
movement, wryneck or torticollis, facial
grimacing, abnormal eye movements,
backward rolling of eyes in the sockets
(oculogyric crisis)
May occur anytime from a
few minutes to several
hours after first dose of
antipsychotic drug
Extrapyramidal side effects
Side Effect Symptoms Onset and prevalence
Tardive dyskinesia
(abnormal movements)
Most frequent serious side effect resulting
from termination of the drug, during
reduction in dosage, or after long-term, high-
dose therapy. Characterized by involuntary
rhythmic, stereotyped movements, tongue
protrusion, cheek puffing, involuntary
movements of extremities and trunk
Occurs in approximately 3% to 5%
of clients taking antipsychotics in
first 10 years
Neuroleptic malignant
syndrome (NMS)
Severe parkinsonian muscle rigidity, very high
fever, tachycardia, tachypnea,
fluctuations in blood pressure, diaphoresis,
and rapid deterioration of mental status to
stupor and
It is a relatively rare, but
potentially fatal, complication of
treatment with neuroleptic drugs.
Onset can occur within hours or
even years after drug initiation, and
progression is rapid over the
following 24 to 72 hours
Management of extrapyramidal effects
• Reduce or discontinue antipsychotic agent; irreversible adverse effect
Give vitamin E,
• Administer anticholinergic agent, such as benztropine mesylate
• Monitor vital signs, degree of muscle rigidity, intake and output, level of
consciousness.
Nursing Implications/ Considerations in administering
Antipsychotics
• Evaluation of blood pressure, complete blood count, liver function tests, and vision tests
before starting therapy and at periodic intervals thereafter as determined by the
prescribing clinician
• If antacids are needed, give them either 2 hours prior to or 1 hour after administration of
the antipsychotic medication(decrease potency)
Nursing Implications/ Considerations in administering
Antipsychotics
• If a single daily dose is ordered, give oral neuroleptics within 1 or 2 hours of bedtime,
whenever possible, to aid sleep.
• Do not give antipsychotic drugs subcutaneously; Administer them as deep intramuscular
injections.
• Use manufacturers specifications in parenteral administration
• Know that antipsychotic agents may provoke seizures in clients with seizure disorders.
Nursing Implications/ Considerations in administering
Antipsychotics
• Closely observe the client receiving antipsychotic drugs for the following:
Therapeutic effects of the drugs, such as decreased agitation, decreased hallucinations,
and increased socialization
A decrease in nausea and vomiting if the drug is given as an antiemetic
Drug-induced EPS
Anticholinergic effects, respiratory depression, and hypersensitivity
Signs of agranulocytosis (eg, sore throat, fever, and discomfort)
Antidepressants
Antidepressants
• Drugs used in the pharmacologic management of depressive disorders are derived three
main chemical groups:
1. Tricyclic antidepressants (TCAs)
2. Monoamine oxidase inhibitors (MAOIs).
3. Selective serotonin reuptake inhibitors (SSRIs)
• SSRI are first line followed by TCA. MAOIs are third line due to interactions with food
containing tyramine and tryptophan
• TCAs can also be used for treating neurotic disorders like nocturnal enuresis.
Mechanisms of Action
• Antidepressant drugs generally act by normalizing abnormal neurotransmission
systems in the brain by altering the amounts of neurotransmitters and the number
or sensitivity of receptors.
SSRIs selectively inhibit the reuptake of serotonin.
MAOIs prevent the metabolism of neurotransmitter molecules..
Tricyclic antidepressants inhibit reuptake of norepinephrine and serotonin.
• These mechanisms thereby increase the amount of neurotransmitter available to
bind to receptors
Mechanisms of Action
For the drugs to be effective:
• Dosage may be divided, but the total dose can be given at bed time due to the sedative
effects.
• Minimum dose should be given then increased gradually.
• Four to six weeks must be allowed to pass for therapeutic effects to be observed.
• Medication needs to be continued for 6 months after patient is free from depression.
Examples of antidepressants
Major Groups Generic Name Trade Name Daily Dosage (range)
Tricyclic antidepressants Amitriptyline Elavil (laroxyl) 75-300mg
Imipramine Tofranil 100-300mg
Monoamine Oxidase
Inhibitors
Isocarboxacid Marplan 10-60mg
Phenelzine Nardil 45-90mg
Selective Serotonin
Reuptake Inhibitors
Fluoxetine Prozac 20mg
Citalopram Cipramil 20-60mg
Side Effects of antidepressants: Some of the side effects that might be
experienced include mild anticholinergic effects from tricyclic and monoamine
oxidase inhibitors: Include;
Dry mouth
 Constipation
 Blurred vision
 Tachycardia
Nausea
 Oedema
Hypotension
Urinary retention
Side Effects of antidepressants
Side effects that are specific to tricyclics are:
• Allergic reactions manifested as skin rash and jaundice.
• Tachycardia.
• Tremors.
• Long term treatment may depress bone marrow, predispose to sore throat and
aching, and fever.
Side Effects of antidepressants
Specific side effects of monoamine oxidase inhibitors include:
• Liver damage that is rare but fatal.
• Precipitation of manic episodes.
• Hypertension crisis characterized by severe headache palpitation, neck stiffness, nausea,
vomiting, increased Bp, chest pain and collapse. It occurs 30 minutes to 24 hours after
eating food containing tyramine and tryptophan. These foods include cheese, wine, beer,
sour cream, liver, chocolate, bananas, avocadoes, soy sauce, and beans.
Contraindications
• The use of antidepressants is contraindicated when the patient suffers from;
 Glaucoma
Agitated states
 Urinary retention
 Cardiac disorders
Seizure disorders
Antidepressant discontinuation syndrome
• Occurs in approximately 20 percent of patients after abrupt discontinuation of an
antidepressant medication that was taken for at least six weeks.
• It is more likely with a longer duration of treatment and a shorter half-life of the treatment
drug.
• All antidepressants are capable of producing symptoms.
Antidepressant discontinuation syndrome
Symptoms
• Flu-like symptoms, insomnia, nausea, imbalance, flashes of lights, "electric shock"
sensations, hyperresponsivity to noises or lights.
Prevention
• Patient education to include warnings about the potential problems associated with abrupt
discontinuation.
• Tailing off the drug
Mood- Stabilizing Agents
(Antimanic drugs)
1. Lithium carbonate
• This is a naturally occurring metallic salt used in the management of bipolar affective
disorder.
• It is more effective in the treatment and prevention of mania than in preventing depression.
Mode of action
• Affect synthesis, release and reuptake of several neurotransmitters in the brain including
acetylcholine, dopamine, GABA and norepinephrine.
• It also stabilizes post synaptic receptor sensitivity to neurotransmitters.
Dose: PO 900-1200 mg daily in divided dosages
Side effects: metallic taste, hand tremors, nausea, polyuria, diarrhea, fatigue, edema and
weight gain.
2. Other mood stabilizers
Valproic acid
• Valproic acid (sodium valproate) is an anticonvulsant indicated for bipolar disorders
Mode of action
• Regulate calcium and sodium channels function leading to enhanced GABA activity and
reduced glutamate activity in the brain
Indications
• Schizophrenic disorder, depression, bipolar disorder, impulse control disorder
Dose
• 10-15mg /KgBW/Day in 2 divided doses
Adverse effects
• Aplastic anemia, hepatitis, exfoliative dermatitis and hypothyroidism
2. Other mood stabilizers
Carbamazine(Tegretol)
• An anticonvulsant chemically related to the tricyclic antidepressants
Indications
• Seizure disorders, neuralgia, unipolar and bipolar disorders
Dose
• 400-1000mg/day in two divided doses
Side effects
• CNS effects e.g. ataxia, drowsiness, sedation; GIT effects like anorexia, nausea,
vomiting; Skin disorders like urticaria, exfoliative dermatitis; blood dyscrasias
like anemia, thrombocytopenia, agranulocytosis; liver damage
Antiparkinsonian Agents Used to Treat Extrapyramidal
Side Effects of Antipsychotic Drugs
Indication
• Used to treat Parkinsonism of various causes and drug-induced extrapyramidal
reactions.
Action
• Restores the natural balance of acetylcholine and dopamine in the CNS.
Contraindications/Precautions
• Contraindicated in individuals with hypersensitivity, Angle-closure glaucoma;
pyloric, duodenal, or bladder neck obstructions; prostatic hypertrophy; or
myasthenia gravis.
• Caution should be used in administering these drugs to clients with hepatic,
renal, or cardiac insufficiency; elderly and debilitated clients; those with a
tendency toward urinary retention; or those exposed to high environmental
temperatures.
Antiparkinsonian Agents Used to Treat Extrapyramidal
Side Effects of Antipsychotic Drugs
Common side effects
• Anticholinergic effects (dry mouth, blurred vision, constipation, paralytic ileus, urinary
retention, tachycardia, elevated temperature, decreased sweating), nausea/GI upset,
sedation, dizziness, orthostatic hypotension, exacerbation of psychoses.
• Examples
• Benztropine (Cogentin) – 0.5-2mgPO,tid;2 mg IV/IM
• Biperiden (Akineton) – 2-6 MG PO tid, 2mg IV/IM
• Trihexyphenidyl (Artane) – 2-5mg PO tid

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Psychopharmacology.pptx

  • 2. Psychopharmacology Introduction • Psychopharmacology is the study of the regulation and stabilization of emotions, behavior, and cognition through the interactions of neurotransmitters and drugs • These drugs are referred to as psychotropic agents or psychoactive or psychotherapeutic drugs.
  • 3. Classification of psychotropic drugs 1. Antipsychotic agents 2. Antianxiety agents (anxiolytics) and hypnotics 3. Antidepressants 4. Antimanic agents 5. Anticonvulsants 6. Anticholinergic or antiparkinsonism agents, which are used to alleviate extrapyramidal symptoms or adverse effects of psychotropic agents
  • 4. The science of psychopharmacology • The science of psychopharmacology focuses on neurotransmission. • Neurotransmitters undergo six steps, each of which offers a potential target for therapeutic intervention by a drug; 1. Synthesis 2. Vesicular uptake 3. Transmitter release 4. Receptor binding 5. Cellular re-uptake 6. Transmitter metabolism.
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  • 6. Antipsychotic Medication • Antipsychotic drugs are also called major tranquillizers or neuroleptics. • Antipsychotic drugs are derived from several chemical groups and broadly categorized as; 1. Typical or traditional phenothiazines 2. Atypical newer drugs. Mode of action • They occupy or block dopamine receptors in the brain thereby decreasing the effects of dopamine. • Antipsychotic effects occur when the drug has been given for a few weeks.
  • 7. Indications • Treatment of schizophrenia and other psychotic disorders. • Selected agents are used in the treatment of bipolar mania • Others uses include; Antiemetics (chlorpromazine, perphenazine, promethazine) Treatment of intractable hiccoughs (chlorpromazine) Control of tics and vocal utterances in Tourette’s disorder (haloperidol, pimozide).
  • 8. Antipsychotic Medication • Manifestations of hyperarousal e.g. anxiety, agitation, hyperactivity, insomnia, aggressive or combative behaviour are relieved more quickly than hallucinations, delusions and thought disorders. • These agents also have antiemetic properties. • Drugs should be given using the following time frame: Six months for first psychotic episode. One year period for second psychotic episode. Indefinite period for third and later psychotic episodes.
  • 9. Categories of antipsychotic drugs 1. Phenothiazines 2. Butyrophenones 3. Thioxanthenes 4. Phenothiazine like 5. Atypical
  • 10. 1. Phenothiazines Generic Name Trade Name Daily Dose Range Chlorpromazine Largactil 300-1000mgs Thioridazine Melleril 50-800mg Acetophenazine Tindal 80-120mg Mesoridazine serentil 100-400mg Promazine sprine 10-200mg Fluphenazine Moditen 2.5-20mg Trifluoperazine Stelazine 5-30mg
  • 11. 2. Butyrophenones Generic Name Trade Name Daily Dose Range Haloperidol Haldol, Serenace 1-20mg 3. Thioxanthenes Thiothixene Navane 6-60mgs Flupenthixol Depixol 6-18mg Zuclopenthixol Clopixol 20-150mg
  • 12. 2. Phenothiazine like Generic Name Trade Name Daily Dose Range Sulpride Domatil,Sulparex 200-2400mg Molindone Lidone 50-400mgs Loxapine Loxitane 60-250mgs Pimozide Orap 2-10mg
  • 13. 5. Atypical Generic Name Trade Name Daily Dose Range Clozapine clozaril 50-900mg olanzapine zyprexa 5-10mg Quetiapine Seroquel 25-50mg Risperodone Risperdal 2-8mg
  • 14. 6. Deport injections Generic Name Trade Name Daily Dose Range Group Fluphenazine decanoate Modecate 12.5-100mg(IM 2 Weekly) Phenothiazines Zuclopenthixol Acetate Clopixol Acuphase 50-150mg every 2-3 days Thioxanthenes Haloperidol decanoate Haldol decanoate 50-300mg (IM 4 weekly) Butyrophenon
  • 15. Contraindications/Precautions Typical antipsychotics are contraindicated in:  Clients with known hypersensitivity (cross-sensitivity may exist among phenothiazines).  Patients in comatose states or when central nervous system (CNS) depression is evident  Blood dyscrasias  Clients with Parkinson’s disease  Narrow angle glaucoma  Liver, renal, or cardiac insufficiency; or those with poorly controlled seizure disorders
  • 16. Side Effects • The effects of these medications are related to blockage of a number of receptors for which they exhibit various degrees of affinity. • Dopamine blockage results in extrapyramidal symptoms (EPS) and prolactin elevation (galactorrhea; gynecomastia). • Cholinergic blockade causes anticholinergic side effects (dry mouth, blurred vision, constipation, urinary retention and tachycardia). • Blockage of the alpha1-adrenergic receptors produces dizziness, orthostatic hypotension, tremors, and reflex tachycardia.
  • 17. Side Effects • Histamine blockade is associated with weight gain and sedation. • Skin reactions such as urticaria, dermatitis, and pigmentation of the skin • Photosensitivity • Gastrointestinal distress such as nausea, heartburn, and jaundice • Decreased libido, retrograde ejaculation, and gynecomastia (men) • Amenorrhea
  • 18. Extrapyramidal side effects • The extrapyramidal system is a biological neural network that is part of the motor system causing involuntary actions. • The system is called extrapyramidal to distinguish it from the tracts of the motor cortex that reach their targets by traveling through the pyramids of the medulla • Antipsychotic medications commonly produce extrapyramidal symptoms as side effects, especially typical ones. • Extrapyramidal symptoms are caused by dopamine blockade or depletion in the basal ganglia; this lack of dopamine often mimics idiopathic pathologies of the extrapyramidal system.
  • 19. Functions of extrapyramidal tract • Control the movement of the eye balls • Control of tone, posture and equilibrium • Control of complex movements of the body and limbs e.g. coordinated movement of arms and legs during walking • Exert tonic inhibition control over the lower centres
  • 20. Extrapyramidal side effects Side Effect Symptoms Onset and prevalence Parkinsonism Motor retardation or akinesia, characterized by masklike appearance, rigidity, tremors, pill rolling, excessive salivation(sialorrhea) Generally occurs after first week of treatment or before second month Akathisia (motor restlessness) Constant state of movement, characterized by restlessness, difficulty sitting still, or strong urge to move about Generally occurs 2 weeks after treatment begins Acute dystonic reactions (disturbance of movement involving the muscles of the head, neck, trunk, or limbs) Irregular, involuntary spastic muscle movement, wryneck or torticollis, facial grimacing, abnormal eye movements, backward rolling of eyes in the sockets (oculogyric crisis) May occur anytime from a few minutes to several hours after first dose of antipsychotic drug
  • 21. Extrapyramidal side effects Side Effect Symptoms Onset and prevalence Tardive dyskinesia (abnormal movements) Most frequent serious side effect resulting from termination of the drug, during reduction in dosage, or after long-term, high- dose therapy. Characterized by involuntary rhythmic, stereotyped movements, tongue protrusion, cheek puffing, involuntary movements of extremities and trunk Occurs in approximately 3% to 5% of clients taking antipsychotics in first 10 years Neuroleptic malignant syndrome (NMS) Severe parkinsonian muscle rigidity, very high fever, tachycardia, tachypnea, fluctuations in blood pressure, diaphoresis, and rapid deterioration of mental status to stupor and It is a relatively rare, but potentially fatal, complication of treatment with neuroleptic drugs. Onset can occur within hours or even years after drug initiation, and progression is rapid over the following 24 to 72 hours
  • 22. Management of extrapyramidal effects • Reduce or discontinue antipsychotic agent; irreversible adverse effect Give vitamin E, • Administer anticholinergic agent, such as benztropine mesylate • Monitor vital signs, degree of muscle rigidity, intake and output, level of consciousness.
  • 23. Nursing Implications/ Considerations in administering Antipsychotics • Evaluation of blood pressure, complete blood count, liver function tests, and vision tests before starting therapy and at periodic intervals thereafter as determined by the prescribing clinician • If antacids are needed, give them either 2 hours prior to or 1 hour after administration of the antipsychotic medication(decrease potency)
  • 24. Nursing Implications/ Considerations in administering Antipsychotics • If a single daily dose is ordered, give oral neuroleptics within 1 or 2 hours of bedtime, whenever possible, to aid sleep. • Do not give antipsychotic drugs subcutaneously; Administer them as deep intramuscular injections. • Use manufacturers specifications in parenteral administration • Know that antipsychotic agents may provoke seizures in clients with seizure disorders.
  • 25. Nursing Implications/ Considerations in administering Antipsychotics • Closely observe the client receiving antipsychotic drugs for the following: Therapeutic effects of the drugs, such as decreased agitation, decreased hallucinations, and increased socialization A decrease in nausea and vomiting if the drug is given as an antiemetic Drug-induced EPS Anticholinergic effects, respiratory depression, and hypersensitivity Signs of agranulocytosis (eg, sore throat, fever, and discomfort)
  • 27. Antidepressants • Drugs used in the pharmacologic management of depressive disorders are derived three main chemical groups: 1. Tricyclic antidepressants (TCAs) 2. Monoamine oxidase inhibitors (MAOIs). 3. Selective serotonin reuptake inhibitors (SSRIs) • SSRI are first line followed by TCA. MAOIs are third line due to interactions with food containing tyramine and tryptophan • TCAs can also be used for treating neurotic disorders like nocturnal enuresis.
  • 28. Mechanisms of Action • Antidepressant drugs generally act by normalizing abnormal neurotransmission systems in the brain by altering the amounts of neurotransmitters and the number or sensitivity of receptors. SSRIs selectively inhibit the reuptake of serotonin. MAOIs prevent the metabolism of neurotransmitter molecules.. Tricyclic antidepressants inhibit reuptake of norepinephrine and serotonin. • These mechanisms thereby increase the amount of neurotransmitter available to bind to receptors
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  • 30. Mechanisms of Action For the drugs to be effective: • Dosage may be divided, but the total dose can be given at bed time due to the sedative effects. • Minimum dose should be given then increased gradually. • Four to six weeks must be allowed to pass for therapeutic effects to be observed. • Medication needs to be continued for 6 months after patient is free from depression.
  • 31. Examples of antidepressants Major Groups Generic Name Trade Name Daily Dosage (range) Tricyclic antidepressants Amitriptyline Elavil (laroxyl) 75-300mg Imipramine Tofranil 100-300mg Monoamine Oxidase Inhibitors Isocarboxacid Marplan 10-60mg Phenelzine Nardil 45-90mg Selective Serotonin Reuptake Inhibitors Fluoxetine Prozac 20mg Citalopram Cipramil 20-60mg
  • 32. Side Effects of antidepressants: Some of the side effects that might be experienced include mild anticholinergic effects from tricyclic and monoamine oxidase inhibitors: Include; Dry mouth  Constipation  Blurred vision  Tachycardia Nausea  Oedema Hypotension Urinary retention
  • 33. Side Effects of antidepressants Side effects that are specific to tricyclics are: • Allergic reactions manifested as skin rash and jaundice. • Tachycardia. • Tremors. • Long term treatment may depress bone marrow, predispose to sore throat and aching, and fever.
  • 34. Side Effects of antidepressants Specific side effects of monoamine oxidase inhibitors include: • Liver damage that is rare but fatal. • Precipitation of manic episodes. • Hypertension crisis characterized by severe headache palpitation, neck stiffness, nausea, vomiting, increased Bp, chest pain and collapse. It occurs 30 minutes to 24 hours after eating food containing tyramine and tryptophan. These foods include cheese, wine, beer, sour cream, liver, chocolate, bananas, avocadoes, soy sauce, and beans.
  • 35. Contraindications • The use of antidepressants is contraindicated when the patient suffers from;  Glaucoma Agitated states  Urinary retention  Cardiac disorders Seizure disorders
  • 36. Antidepressant discontinuation syndrome • Occurs in approximately 20 percent of patients after abrupt discontinuation of an antidepressant medication that was taken for at least six weeks. • It is more likely with a longer duration of treatment and a shorter half-life of the treatment drug. • All antidepressants are capable of producing symptoms.
  • 37. Antidepressant discontinuation syndrome Symptoms • Flu-like symptoms, insomnia, nausea, imbalance, flashes of lights, "electric shock" sensations, hyperresponsivity to noises or lights. Prevention • Patient education to include warnings about the potential problems associated with abrupt discontinuation. • Tailing off the drug
  • 39. 1. Lithium carbonate • This is a naturally occurring metallic salt used in the management of bipolar affective disorder. • It is more effective in the treatment and prevention of mania than in preventing depression. Mode of action • Affect synthesis, release and reuptake of several neurotransmitters in the brain including acetylcholine, dopamine, GABA and norepinephrine. • It also stabilizes post synaptic receptor sensitivity to neurotransmitters. Dose: PO 900-1200 mg daily in divided dosages Side effects: metallic taste, hand tremors, nausea, polyuria, diarrhea, fatigue, edema and weight gain.
  • 40. 2. Other mood stabilizers Valproic acid • Valproic acid (sodium valproate) is an anticonvulsant indicated for bipolar disorders Mode of action • Regulate calcium and sodium channels function leading to enhanced GABA activity and reduced glutamate activity in the brain Indications • Schizophrenic disorder, depression, bipolar disorder, impulse control disorder Dose • 10-15mg /KgBW/Day in 2 divided doses Adverse effects • Aplastic anemia, hepatitis, exfoliative dermatitis and hypothyroidism
  • 41. 2. Other mood stabilizers Carbamazine(Tegretol) • An anticonvulsant chemically related to the tricyclic antidepressants Indications • Seizure disorders, neuralgia, unipolar and bipolar disorders Dose • 400-1000mg/day in two divided doses Side effects • CNS effects e.g. ataxia, drowsiness, sedation; GIT effects like anorexia, nausea, vomiting; Skin disorders like urticaria, exfoliative dermatitis; blood dyscrasias like anemia, thrombocytopenia, agranulocytosis; liver damage
  • 42. Antiparkinsonian Agents Used to Treat Extrapyramidal Side Effects of Antipsychotic Drugs Indication • Used to treat Parkinsonism of various causes and drug-induced extrapyramidal reactions. Action • Restores the natural balance of acetylcholine and dopamine in the CNS. Contraindications/Precautions • Contraindicated in individuals with hypersensitivity, Angle-closure glaucoma; pyloric, duodenal, or bladder neck obstructions; prostatic hypertrophy; or myasthenia gravis. • Caution should be used in administering these drugs to clients with hepatic, renal, or cardiac insufficiency; elderly and debilitated clients; those with a tendency toward urinary retention; or those exposed to high environmental temperatures.
  • 43. Antiparkinsonian Agents Used to Treat Extrapyramidal Side Effects of Antipsychotic Drugs Common side effects • Anticholinergic effects (dry mouth, blurred vision, constipation, paralytic ileus, urinary retention, tachycardia, elevated temperature, decreased sweating), nausea/GI upset, sedation, dizziness, orthostatic hypotension, exacerbation of psychoses. • Examples • Benztropine (Cogentin) – 0.5-2mgPO,tid;2 mg IV/IM • Biperiden (Akineton) – 2-6 MG PO tid, 2mg IV/IM • Trihexyphenidyl (Artane) – 2-5mg PO tid