Antipsychotic and Antiparkinsonian Drugs PDF

ARAB REPUBLIC OF EGYPT MINISTRY OF HIGHER EDUCATION KFR ELSHIKEUNIVERSITY FACULTY OF NURSING  Introduction to psychopharmacology  Antipsychotic medications  History  Indications  Contraindications  Mechanism of action  Classification of Antipsychotics  Drug Int...

ARAB REPUBLIC OF EGYPT MINISTRY OF HIGHER EDUCATION KFR ELSHIKEUNIVERSITY FACULTY OF NURSING  Introduction to psychopharmacology  Antipsychotic medications  History  Indications  Contraindications  Mechanism of action  Classification of Antipsychotics  Drug Interaction  Side Effects and its Nursing Intervention  Teaching patients and family Antiparkinsonian drugs  Main indication  Contraindication  Classification  Mechanism of action  Teaching patient  Nursing action  Nursing implication  Psychopharmacology means the study of chemistry, deposition, actions, and clinical pharmacology of drugs used to treat psychiatric disorders.  The brain consists of neurons. Neurons or nerve cells comprise the basic unit of the nervous system. Nerve cells or neurons are designed to receive and give information.  Neuron composed of dendrites (projection from the neuron), cell body, axon and axon terminal buttons.  Dendrites receive information and transmit it to the cell body. Axons send information from the nerve cell to the dendrites from next neuron.  It is a junction between one nerve and another. It is the space where the electrical intracellular signal becomes a chemical extracellular signal.  Neurotransmitters are synthesized from natural precursors (e.g. amino acids) in the body.  Stored in storage vesicles in the presynaptic terminals of the cell.  Neurotransmitters are classified into: A. Excitatory neurotransmitters reduce the membrane potential and enhance the transmission of the signal between neurons. B. Inhibitory neurotransmitters slow down the transmission of the signal between neurons.  Dopamine (excitatory transmitters) is important in conceptualizing the pathology and treatment of schizophrenia and Parkinsonism.  Gamma Aminobutyric Acid (GABA) (inhibitory transmitters) is important in conceptualizing the pathology and treatment of anxiety.  Norepinephrine (excitatory transmitters) is important in conceptualizing the pathology and treatment of mania and depression.  Serotonin (excitatory transmitters) is important in conceptualizing the pathology and treatment of mania and depression.  Acetylcholine (Ach) (excitatory transmitters) is important in conceptualizing the pathology and treatment of Alzheimer's disorder and Parkinsonism.   Specific proteins intended to respond to a chemical (i.e., neurotransmitters normally present in blood , tissues or drugs ).  When drugs attach to a receptor, they can act as: A. Receptor agonist: A receptor agonist is a drug that fits and activates the receptor in the same manner as the naturally occurring. B. Receptors antagonists: substances that block the response of given receptors and compromise the receptor's function.  Toxicity:  The point at which concentrations of the drug in the blood stream is high enough to become harmful or poisonous to the body.  Therapeutic index:  It is the ratio of the maximum nontoxic dose to the minimum effective dose. There are dugs with a high therapeutic index and drugs with a low therapeutic index (drugs have a narrow range).  Target symptoms:  They are the specific symptoms that medication aims to alter.  Half life:  The time required for normal biologic processes to metabolize or eliminate half the quantity of a drug or other substance.  polypharmacy:  The use of two or more psychotropic drugs , two or more drugs of the same chemical class, or two or more drugs with the same or similar pharmacologic actions to treat different conditions.  Efficacy :  The degree to which a drug can cause the desired response. Potency:  The amount of the drug needed to achieve the therapeutic effect. So low potency drugs need to be given in higher dose and vice versa. OR the ability of the drug to reduce symptoms and disorder Pharmacodynamics: (How does the drug act on the body)  The actual biological and physiological effects on living tissue that are caused by the interaction of drug with tissue receptors. Pharmacokinetics:-  It refers to the effects that the body has on drug.  Absorption:- getting the drug into blood stream.  Distribution: - getting the drug from blood stream to tissue or organs, psychotropic drugs are bound largely to protein and pass easily to brain.  Metabolism:- breaking the drug down into an inactive and typically water- soluble form. Most psychotropic drugs are metabolizes partially in the liver.  Excretion:- getting the drugs out of the body.   Antipsychotics are also referred to as major tranquilizers (because they produce calmness), neuroleptics (because they produce neurologic symptoms) or dopamine receptor antagonists (because they block dopamine receptors).  History:  Antipsychotics were discovered accidentally around 1950.  Chlorpromazine is considered the first antipsychotic drug.   hallucination and delusion. Psychiatric uses Nonpsychiatric uses Schizophrenia Nausea and vomiting. Acute mania  Intractable hiccups. Some resistant bipolar Dementia with psychotic symptoms. Severe obsessive compulsive neurosis. Aggressive and sociopathic personality  Cardio vascular disease especially MI  Hypotension or hypertension.  Epilepsy.  Liver disease & Jaundice (as it causes obstructive Jaundice)  Parkinson's disease.  CNS depressant.  Hypersensitivity to drug  As generally, antipsychotic drugs work by blocking of dopamine receptors in the post synaptic thus lead to reduce dopamine activity in the brain.   I- First classification :According to chemical class. Chemical class Generic name Trade name 1-Phenothiazine Clorpromazine (Thorazine) A- Alphatic Clorpropmide (Largactil) B- Piperidine Thioridazine (Mellaril) C- Piperazine Trifluoperazine (Stelazine) Fluphenazine (Prolixion) Perphenazine (Trilafon) ( Haldol ) 2- Butyrophenones Haloperidol (Safinase) 3-Miscellaneous Thiothixene (Navane) Clozapine (Clozaril) Respridone (Risperdal)  According to ''typicality'' or ''generation'' :- 1-Typical antipsychotics  Typical antipsychotic drugs are further divided based on potency into:  High potency drugs.(Low dose + Low sedation + High EPSEs.  Moderate potency drugs.(Moderate dose +Moderate sedation + High EPSEs.  Low potency drugs.(High dose +High sedation +Low EPSEs 2- Atypical antipsychotics (Second generation)  Atypical antipsychotics differ from typical :-  Reduced or no risk for EPSEs.  Increased effectiveness in treating negative or cognitive symptoms or both.  Efficacy for patients who are unresponsive to typical antipsychotics.  Absence of prolactin elevation and the associated side effect.  3-Novel antipsychotics (Third generation)  Novel antipsychotics are dopamine system stabilizers. This drug has a stabilizing and modulating effect on brain dopamine. This means the drug is intended to reduce dopamine transmission when it too high and to preserve it when is too low.  Drug name Usual Dosage Range (mg/day) Extra pyramidal side effects (EpSE) 1- Typical (First generation) A-High-Potency drug  Fluphenazine (Prolixin) 3-45 ++++  Haloperidol (Haldol ) 2-40 B-Moderate –Potency drug  Pherphenazine (Trilafon) 12-60 +++ C -low-potency drug  Chlorpromazine (Thorazine) 150-1500 ++  Thioridazine (Mellaril) 150-800 2-Atypical (second generation)  Clozapine (Clozaril) 150-600  Risperidone (Risperdal) 2-8 + or -  Olanzapine (Zyprexa) 5-20  Quetiapine(Seroquel) 150-750  Ziprasidone (Geodon) 40-160 3-Novel (Third generation) - Aripiprazole (Abilify )  oral and injectable forms.  Injectable forms :- (Depot form-injection)  It is long acting oil based medication form for the purpose of slow release of drug over several weeks.  * Typical agents  Haloperidol decanoate (Haldol Decanoate)  Usual dose range: 50: 300 mg IM  Usual duration: 3-4 weeks  Fluphenazine decanoate (Prolixion Decanoate)  Usual dose range: 12.5 to 50.0 mg IM  Usual duration: 2-3 weeks  Modecate (every two weeks)  *Atypical agents  Respridone (Risperdal Consta (every 2 weeks) ).  Drug Name Interaction  Sedation drugs and alcohol ↑ C N S depression.  Antacids ↓ The absorption of antipsychotics.  Antidepressants ↑ The plasma level of antidepressant and Antipsychotics.  Anticholienrgic drugs ↑ The risk of atropine psychoses.  Cigarette smoking ↑ Hepatic metabolism of antipsychotics so requiring more doses of antipsychotics.  Antihypertensive drugs. ↑ Profound hypotension.  7. benzodiazepine ↑ C N S depression  8.lithium ↓ Antipsychotic effect  9.Insulin Control of diabetes is weakened  Atropine Toxicity  It is an emergentic situation which cause anticholinergic properties of the antipsychotic which develop signs and symptoms as: Purposeless over activity Agitation Confusion Disorientation Dry and flushed skin Tachycardia Dilated pupils Memory impairment.  Side Effects of Antipsychotics  1-Extra pyramidal side effects (EPSEs) o Early EPSEs: It is reversible Antiparkinson drug A-Dystonia: First choice:  Onset:-usually occur within 48hours after - (e.g., Diphenhydramine beginning of treatment but may occur anytime. (Benadryl) antihistamine  More common in young man. Second choice  Symptoms: characterized by muscular rigidity - (e.g.,Benztropine (Cogentin) due to abnormal tonic groups. Prevent further dystonias with  Torticollis: Stiffness of the neck. anticholinergic agents  Occulogyric crisis: the eye upward lateral Lower dosage or switch to other movement. antipsychotics  Opisthotonos: spasm of the neck and back, the result in arching of the back.  Writers cramp: fatigue spasm affecting hand.  Involuntary protrusion of the tongue.  Peroral spam: Spam of the jaw. B-Drug – Induced Parkinsonism  Anticholinergic Trihexyphenidyl (psedoparkinsonism) (Artane) or benztropine (Cogentin).  Onset: 5-30 days.  Depaminergic agent Amanatidine  Symptoms: Stooped posture, shuffling (Symmeterl) may be also prescribed. gait, drooling, mask like face, tremors, muscle rigidity, slow movement and loss of association C-Akathisia :-  Onset : 5-30 days  Physcian may change antipsychotic.  Symptoms: Subjective motor  Antiparkinsonian drugs (Cogentin – restlessness, patient can't sit for a Artane). while, an argue to paces, a need to  Inderal, Ativan or Valum may be used shift weight from one foot to anther and inability of patient to sit or stand still. o Late EPSEs Anticholinergic agents will worsen TD. (Tardive dyskinesia): (cause: dopamine hypersensitivity) Tardive means ''late appearing'' It is irreversible  Onset: usually developed after 6 months or more.  Symptoms: involuntary, repeated movements of the muscle of the faces, trunk and limbs. Face: protrusion and rolling tongue. Puffing of faces. Grinding of teeth and chewing. Smacking movement. Plinking of the eye. Trunk: twitching of trunk, leg and arms. Shrugging of the shoulder. Limbs: rapid purposeless and irregular movement. Toe movement and foot lapping. 2-Neuroleptic malignant syndrome ( 1-As prophylactic  Nurse should be alert to for this potentially fatal NMS) side effect. It is life threating. 1% of patients taking  Routine taking vital signs.  Encourage adequate water intake among antipsychotics will develop this problem but patients on antipsychotics. 5% to 20% of those will die without 2- As therapeutic treatment.  Immediate stopping to antipsychotic.  Onset: Anytime during the course  Bomocriptine can relieve muscle rigidity.  Dantrolene (Dantrum) may reduce muscle of treatment spasm.  Symptoms: Altered level of  Transfer patient to medical unite consciousness. Supportive measures :-  Cool body to reduce fever.  Hyperthermia.  Maintain hydration with oral and Iv fluids.  Autonomic dysfunction: -  Correct electrolyte imbalance. hypertension, tachycardia,  Frequent monitoring for vital signs. diaphoresis and incontinence. Antipsychotics should not be reinstituted for at least 2 weeks after complete resolution of NMS symptoms.  Muscular rigidity. 3-Anticholienrgic effects: - Encourage high-fiber diet. - Increase water intake. - Encourage increase physical activity. A-Constipation - Give laxatives as ordered. B-Dry mouth - Sip of water frequently. - Provide sugarless candies and gum. - Mouth care. C-Blurred vision - Advice client to avoid potentially dangerous tasks such as driving care. - Clear small items from pathway to prevent falls. D-Urinary hesitation - Provide privacy. - Run water in the sink. Run warm water over the perineum - Avoid prolonged exposure to sunlight. 4-Photo sensitivity - Wear sunscreen on the skin whenever the patient is (increased sensitivity to the effects of the sun) outdoors. Skin eruptions, severe sun burn, blue-gray metallic Advice patient to wear sunglasses outdoor if possible. discolorations over the face and hands 5-Ant adrenergic effect: - Ask client to get out of bed or chair slowly. - Client should sit on the side of the bed for 1 Hypotension or orthostatic full minute while dangling feet and then hypotension slowly rise. - Monitor blood pressure lying and standing at each shift. - If hypotension is a problem, measure blood pressure before each dose is given. B- Weight gain -Caloric controlled diet. - Weight patients every other day. - Provide opportunity for physical exercise. 7-Cardiac effect - Electrocardiogram monitoring is becoming increasingly important Tachycardia 8- Sedation - Advise patient to avoid dangerous tasks when experiencing sedative effect. It is an induced state of quite, -Help patient get up early and involved in calmness or sleep. activities during day to prevent sleep during the day. 9-Seizure  Seizure occurs in D - Document and report any approximately 1% of clients seizure receiving antipsychotics. activity. The antipsychotic medications tend - If a seizure occurs to decrease the seizure threshold. discontinuing antipsychotic may be necessary. 10- Agranulocytosis (A high incidence of agranulocytosis is -Nurse should be alert to the symptoms associated with clozapine treatment) of  It is a life threatens decrease in agranulocytosis. white blood cell. Symptoms: -White blood cells (WBC) should be sore throat, fever, malaise, performed weekly. mouth sore. -Doctors and nurse should follow the Laboratory test: absolute neutrophile role of protocol of clozapin therapy count (ANC) Less than 500/mm3 1-The normal white blood cells (WBC) count is above 3500/mm3 and the absolute neutrophil count (ANC) is 2000/mm3 or higher. 2- if the base line WBCand ANC count are lower than 3500/mm3 and 2000/mm3 , respectively, don’t start clozapine. 3- once started, monitor the WBC count weekly. 4- if WBC and ANC levels are normal for 6 months , monitor level every 2 weeks. 5- if WBC and ANC levels are normal for 1 year, monitor monthly. 6- if WBC levels drop below 3000/mm3 , or the ANC is below 1500/mm3 , clozapine should be discontinued. Monitoring the WBC count and ANC should be performed daily. 7- if no sign of infection is present, clozapine therapy can be resumed once the WBC count is higher than 3000/mm3 and the ANC is higher than 1500/mm3. 8- if the WBC count drops below 2000/mm3 and the ANC is below 1000/mm3 , clozapine should be permanently discontinued.  Help patients understand that several weeks of drug use may be necessary before a benefit is received.  Avoid abrupt withdrawal of medication because EPSEs can occur.  Immediately report signs of sore throat, malaise, fever, or bleeding these signs may indicate a blood dyscrasis.  Caution clients to avoid alcoholic beverages while taking antipsychotic medications.  Caution clients should avoid taking antacids during antipsychotic therapy because antacids might decrease the absorption of antipsychotic drugs.  Advice patients and their family to follow nursing intervention to side effects of the drug.  Avoid immersion in hot water because hypotension may occur, causing falls.  Dress appropriately in hot weather and drink plenty of water to avoid heatstroke.  Good oral hygiene should be practiced to avoid mouth infection and dental caries.  Warn clients to avoid driving or operating hazardous equipment and notify the physician if vision changes or sedation occur.  Keep medication away in reach of children hand.  Use sunscreen to prevent sunburn& wear protective clothes when spending time outdoors.  1. Extrapiramidal side effects (EPSEs): are serious and some time dangerous complication of antipsychotic drug, EPSEs caused by blockage of dopamine receptors this lead to imbalance between acetylcholine and dopamine.  2.Parkinson's disease (PD): Is a progressive chronic degenerative disease of unknown cause that involves the area of the brain called extrapyramidal system. This area responsible about normal coordination of involuntary'movement. (PD) caused by a decline in dopamine production. A deficiency in dopamine result in imbalance between a acetylcholine and dopamine.  3. Tremor secondary to lithium or antidepressant drug   Anticholinergic are contraindication in: 1. Glucoma. 2. Gastro-intestinal obstruction. 3. Prostatic hypertrophy. 4. Urinary bladder neck obstruction or duodenal obstruction. 5. Used with caution in client with cardiovascular disorders, during pregnancy, and older patients.  Dopaminergic agents are contraindicated in: 1. Hypersensitivity to specific -drug (Such as MAOI) 2-Narrow-angle glaucoma. 3- Breastfeeding  1- Anticholinergic drugs  Trihexphenidyl (Artane)  Benztropine (Cogentin)  Biperdin (Akineton)  Treating parkinsonism by decrease acetylcholine.  2-Anticholinergic antihistaminic  Diphenhydramine (Benadryl)  3- Dopaminergic drugs  Levodopa ( Amantadine )  Larodopa (Symmetrel)  Treat Parkinsonism by increasing dopamine.  4- Beta blocker  Atenolol  pindolol  1- Anticholinergic drugs inhibit acetylcholine, these drug also inhibit reuptake of dopamine. Both of these effects contribute to the restoration of acetylcholine-dopamine balance.  2-Dopaminergic drugs increase dopamine level.  Extrapyramidal side effects treated only with anticholingeric drugs which these drug work by restoring_ imbalance (Ach-dopamine balance) caused by antipsychotic drug.  Extrapyramidal side effects not treated with dopaminergic drugs because psychosis is thought to be related to an increase dopamine level. if these drugs give to schizophrenic patients, the psychotic symptoms might be increase.  Parkinson's disease is treated with antiparkinsonian agents that increase dopamine, or with antichonlinergic drugs or both.  Side effects Nursing intervention 1 Dry mouth - Offer sugarless hard candy and chewing gum. - Take medication before meals 2 Nasal congestion Recommend over the counter nasal decongestant, if approved by physician. 3 Urinary hesitation Introduce running water, privacy, warm water over perineum. 4 Urinary retention Catheterize for residual fluids, encourage frequent voiding. 5 Blurred vision Provide reassurance (normal vision typically returns in sunglasses, advise caution encourage a few weeks), when driving. 6 Constipation Give laxatives as ordered encourage diet with roughage; recommend 3000 to 3500 ml of water per day. 7 Mydriasis If eye pain develops, undiagnosed narrow angle glaucoma may be cause immediate attention is warranted 8 Orthostatic hypotension Request patient to get out of bed slowly, to sit on the edge of the bed a short while, and rise slowly. 9 Sedation Help patient get up early and to get the day started & give medication at bet time. 10 Decreased sweating Ensure that patient remain in cool environment and take adequate fluid.  1. Give antiparkinsonian agents with or immediately often food intake to prevent or reduce gastro-intestinal distress.  2. Observe for therapeutic effects such as decrease salivation, tremor,  3. Observe for improvement in gait, balance, posture, speech, and self-care ability.  4. Monitor for adverse effects due to anti-cholinergic drugs such as dry mouth, constipation, urinary retention.  5. Over dose of anti-cholinergic drugs may result in CNS hyper stimulation (confusion, excitement, hyper pyrexia, agitation, disorientation.) or C.N.S. depression (drowsiness, sedation, coma.... ) then the nurse must be aware of therapeutic range of doses,  - Benztropine 1-4 mg daily.  - Biperiden 2 mg.  - Trihexphenidyl start with 1 mg/ daily and increase usual dose range 5- 15 mg/day. 1. Avoid discontinuing these drug abruptly. 2. Avoid driving or other hazardous activities until drowsiness and blurred vision diminish. 3. Maintain adequate amount of fluid intake (2000-3000 C.C) daily unless contraindication) to prevent excessive dryness of the mouth. Taking the medication just before meals, chewing gum. 4. Report any side effects or unusual symptoms to the physicians or 5. psychiatrist. 6. Limit use of alcohol, high protein food, and vitamin B6 because they decrease the therapeutic effect of levodopa. 7. Avoid over-the counter medication (e.g. cough and cold preparation) that have anti-cholinergic or anti histamine properties and alcohol which C.N.S. depressant, and antacids which will interfere absorption of anti -cholinergic. Thank you