Psychopharmacology: Neurotransmitters, Drugs and Side Effects PDF

PSYCHOPHARMACOLOGY Definition of Terms AXON –part of a neuron that transmits impulses away from the cell body BLOOD-BRAIN BARRIER – a barrier that guards the brain from fluctuations in body chemistry. It regulates the amount and speed with which substances in the blood enter the brai...

PSYCHOPHARMACOLOGY Definition of Terms AXON –part of a neuron that transmits impulses away from the cell body BLOOD-BRAIN BARRIER – a barrier that guards the brain from fluctuations in body chemistry. It regulates the amount and speed with which substances in the blood enter the brain DENDRITES- part of the neuron that transmits impulses toward the cell body LIPID SOLUBILITY – ability of a substance to dissolve in fat NEUROTRANSMITTERS – chemical substances in the nervous system that facilitate the transmission of nerve impulses across synapses between neurons SYNAPSE- microscopic space between two neurons VESICLE – storage sac at the synaptic terminal NEURONS (nerve cells) Receive and give information through axons and dendrites Information, in the form of electrochemical excitation cell body axon presynaptic terminal; neurotransmitters are stimulated released from the presynaptic terminal synaptic cleft combine with postsynaptic receptors causing neuronal response NEUROTRANSMITTERS Protein Amino acids in the bloodstream Synthesized in the cell Neurotransmitters Stored in storage vesicles in the presynaptic terminals  Neurotransmitters are inactivated in 2 ways: 1. Metabolized by enzymes 2. Taken back into the presynaptic storage vesicles (reuptake) Psychotropic drugs can affect neurotransmitters in several ways DR (drug + receptor) - combining of psychotrotopic drugs with a receptor and prevent the “natural” neurotransmitter from combining with it. E.g. antipsychotics block dopamine) RR (receptor’s reaction)-affect the response of a receptor to a neurotransmitter. E.g. TCAs “down-regulate” postsynaptics receptors thus changing these receptors’ sensitivity to neurotransmitters NR (neurotransmitter’s release) - release of a neurotransmitter can be affected e.g. Amantadine (Symmetrel), an antiparkinson drug causes the release of the neurotransmitter dopamine) NA (neurotransmitter’s activation)-terminate the inactivation of neurotransmitters e.g. TCAs block the reuptake of neurotransmitters; MAOIs block enzymatic reduction of neurotransmitters Which one of the following neurotransmitters is altered in depression? A. acetylcholine B. serotonin C. dopamine D. histamine  MOST IMPORTANT NEUROTRANSMITTERS D-opamine-is important in conceptualizing the pathology and treatment of Schizophrenia and Parkinsonism A-cetylcholine –is important in conceptualizing the pathology and treatment of Alzheimer’s disease and Parkinsonism N-orepinephrine –is important in conceptualizing the pathology and treatment of Mania and Depression G-ABA (gamma-aminobutyric acid) –is important in conceptualizing the pathology and treatment of Anxiety S-erotonin- is important in conceptualizing the pathology and treatment of Mania and Depression DOPAMINE “BET ME C.M.” Brain stem – primary location Excitatory- general function Tyrosine- where dopamine is synthesized Movements- complex, controlled by dopamine Emotion-area of control Cognition-area of control Motivation-area of control ACETYLCHOLINE Location-Brain, Spinal Cord, PNS, Skeletal muscles Other Functions- Sleep-wake cycle,Activation of muscles General Function- Excitatory &Inhibitory Synthesis- Choline (red meat & vegetables) NOREPINEPHRINE Location- Brain stem Other functions-changes in attention, learning and memory, sleep and wakefulness, mood regulation General Function- excitatory Synthesis- tyrosine GABA Major inhibitory neurotransmitter Amino acid Modulate other neurotransmitters SEROTONIN “BEST TIPS F” Brain -location Emotions- function Sleep and wakefulness- function Temperature regulation- function Tryptophan- synthesis (e.g. gatas) Inhibitory- general function Pain control- function Sexual behavior- function Food intake control- function Increase in dopamine --------schizophrenia Decrease in norepinephrine---depression Decrease in serotonin-----------depression Decrease in acetylcholine------alzheimer’s Decrease in GABA --------------anxiety ANTIPARKINSON DRUG SOME TERMS Anticholinergic effect- caused by drugs that block acetylcholine receptors (dry mouth, blurred vision) Basal ganglia- subcortical structures that fine- tune involuntary movement, including the caudate nucleus, putamen and globus pallidus Exrtrapyramidal system- outside the voluntary (pyramidal) tract; coordinates involuntary movements Extrapyramidal side effects – caused by drugs that block dopamine, creating a dopamine- acetylcholine imbalance Substantia nigra- black substance; a pigmented area in the midbrain where dopamine is synthesized Extrapyramidal system- lies infront of the pyramidal system in the premotor area of the frontal lobe and extends to the basal ganglia and midbrain Deficiency of dopamine and decrease in dopamine transmission to the basal ganglia in the extrapyramidal system causes malfunction Imbalance of dopamine with another neurotransmitter, acetylcholine causes parkinsonism Balance of dopamine and Ach enables the extrapyramidal system to control posture, balance, walking and other movements  A parkinsonian imbalance can occur in these three ways: 1. Brain may produce less dopamine as in degeneration of the substantia nigra in parkinson’s disease 2. Neuronal dopamine can be depleted chemically with reserpine( formulated in 1953 which is effective in treating psychosis but causes severe depression by depleting norepinephrine) 3. Dopamine can be blocked at the postsynaptic receptor as occurs with antipsychotics *when imbalance occurs, motor neurons experience a continual “switched on’ effect without the switching off needed for normal movement Imbalance causing parkinsonism D ACh  Balance is accomplished in three ways: 1. Drugs are used to increase the level of dopamine (dopaminergic agents) 2. Drugs are used to decrease the level of Ach (anticholinergic agents) 3. A combination of these two drugs is used to increase dopamine and decrease Ach simultaneously DOPAMINERGIC DRUGS INCREASE DOPAMINE AVAILABILITY 1. dopamine precursor –levodopa (Dopar, Larodopa); carbidopa-levodopa(sinemet) 2 dopamine releaser –Amantadine (symmetryl) 3. Dopamine receptor agonist- Bromocriptine(Parlodel); Pergolide (Permax) 4. Dopamine- metabolism inhibitor – Selegiline(Eldypryl) ACh D ANTICHOLINERGIC DRUGS DECREASE ACETLYCHOLINE AVAILABILITY Trihexyphenidyl (Artane); Benztropine (Cogentin); Biperiden (Akineton); Diphenhydramine (Benadryl); Ethopropazine (Parsidol); Procyclidine(Kemadrin) ACh D  Dopaminergic Drugs To live (Levodopa), you need a car (carbidopa) and a man (Amantidine) not your brother (bromocriptine) per (pergolide) se (selegiline) ANTI-CHOLINERGIC BACPAK ( BENADRYL, ARTANE, COGENTIN, PARSIDOL, AKINETON, KEMADRIN) (di-tri-ben-etho-bi-pro) SIDE EFFECTS AND NURSING INTERVENTIONS FOR ANTICHOLINERGICS CNS- sedation: help patient get up early and get the day started EYES-Blurred vision, photophobia: reassurance (normal vision typically returns in a few weeks); sunglasses, caution when driving, tolerance develops -Mydriasis: if eye pain develops could indicate undiagnosed narrow angle glaucoma-immediate attention is warranted NOSE-Nasal congestion: OTC nasal decongestant if approved by physician MOUTH-Dry mouth : sugarless hard candy and chewing gum; frequent rinses; take before meals HEART-tachycardia, palpitations-report to physician -Orthostatic hypotension: request patient to get out of bed slowly, to sit on the edge of the bed a short while and rise slowly URINARY TRACT-Urinary hesitation: running water, privacy, warm water over perineum Urinary retention: catheterize for residual fluids, encourage frequent voiding DIGESTIVE- Constipation: laxatives as ordered, diet with roughage, 2500 to 3000 ml water per day SKIN-Decreased sweating- this can lead to fever; take temperature; if fever occurs, reduce body temperature Temperature: limit strenuous activity, wear appropriate clothing ANTIPSYCHOTICS HISTORY Chlorpromazine (Thorazine) –first antipsychotic drug; from the phenothiazine family of drugs; proved quite sedating (tendency to sleep); historically refered as major tranquilizers  ANTIPSYCHOTICS (TYPICAL) =12 “LAPIT CA MAMA, FAHATID CITA” –GENERIC NAMES L-LOXAPINE (LOXITANE) P-PHERPHENAZINE (TRILAFON) T-TRIFLUOPERAZINE (STELAZINE) C-CHLORPROMAZINE (THORAZINE) M-MESORIDAZINE(SERENTIL) M-MOLINDONE (MOBAN) F-FLUPHENAZINE (PROLIXIN) H-HALOPERIDOL (HALDOL) T-THIORIDAZINE (MELLARIL) D-DROPENIDOL (INAPSINE) C-CHLORPROTHIXENE (TARACTAN) T-THIOTIXENE (NAVANE) “LOX.! TRILA STELA THO SER MO, PRO HA, ME INA. TARA NA!” (LOOK! TILA STELA TONG SIR MO, PERO HA, ME INA. TARA NA!) – CORRESPONDING BRAND NAMES  ATYPICAL (7) “A QUIZ SCORE”- generic names A- ARIPIPRAZOLE (ABILIFY) Q-QUETAPINE (SEROQUEL) Z-ZIPRASODONE (ZELDOX) S-SERTINDOLE( SERLECT) C-CLOZAPINE (CLOZARIL) O-OLANZAPINE (ZYPREXA) R-RESPIRIDONE(RESPIRDAL ) “Abi, sero ze ser clo zy res”-corresponding brand names CLASSIFICATION OF TRADITIONAL (TYPICAL) ANTIPSYCHOTIC DRUGS BASED ON POTENCY HIGH-POTENCY: Fluphenazine (Prolixin); Haloperidol(Haldol); Thiotixene(Navane); Trifluoperazine(Stelazine) MODERATE-POTENCY: Loxapine(Loxitane); Molindone (Moban); Perphenazine(Trilafon) LOW-POTENCY: Chlorpromazine(Thorazine); Chlorprotixene(Taractan); Mesoridazine(Serentil); Thioridazine(Mellaril) High-potency Dosage EPSEs Anti orthostasis sedation range/ cholinergic day fluphenazine 0.5-20 severe mild mild mild haloperidol 1-15 severe mild mild mild thiothixene 8-30 severe mild mild mild trifluoperazine 2-80 severe mild mild mild drugs Dosage EPSEs Anti orthostasis sedation range/ cholinegic day loxapine 20-250 severe mild moderate moderate molindone 50-255 severe mild mild mild perphenazine 12-64 severe mild mild mild Drug Dosage EPSEs Anti Orthostasis Sedation range/ cholinergic day chlorpromazine 30-800 modera moderate severe significant te Thioridazine 150-800 mild severe severe significant chlorprothixene 75-600 modera moderate moderate significant te  ATYPICAL Drug Dosage EPSEs Anti Orthostasis Sedation Effect on range/ cholinergic Negative mg Symptom Clozapine 300- mild severe severe significa significant 900 nt risperidone 4-16 mild mild mild mild significant olanzapine 5-20 mild mild mild moderat significant e quetiapine 300- Mild to mild mild mild significant 400 low sertindole 12-24 Mild to Mild to mild mild significant low moderate ziprasidone 80-160 mild mild mild mild significant  Different Dopaminergic Tracts in the Brain Mesocortical system Involved in negative schizophrenia Mesolimbic system substantia nigra Involved in positive schizophrenia (synthesis of dopamine) Tuberoinfundibular system Involved in neuroendocrine control Nigrostriatal system Involved in extrapyramidal disorders Effect of antipsychotic to 4 dopaminergic tracts NIGROSTRIATAL SYSTEM: (midbrain, thalamus, hypothalamus) -pseudoparkinsonism or extrapyramidal effect TUBERINFUNDIBULAR SYSTEM: (midbrain, hypothalamus) -dopamine inhibition of the hypothalamic hormone prolactin is lifted and can lead to gynecomastia and galactorrhea MESOLIMBIC SYSTEM: (midbrain to limbic forebrain) -a decrease in the symptoms of schizophrenia (positive) MESOCORTICAL SYSTEM: (neocortex to midbrain) -disorder can be worsened in some patients like Risperidone is thought to antagonize serotonin receptors in the cortex thus liberating dopamine-contributing to negative symptoms Positive symptoms- attributed to too much dopamine in the limbic area (hyperactive mesolimbic tract) Negative symptoms-attributed to too little dopamine in the cortex (hypoactive mesocortical tract) INTENDED EFFECTS S-edation-decreases insomnia, for agitation, combative persons E-motional quieting D-ecreases confusion and clouding, hallucinations, delusions and illusions A-mbivalence reduced T-houghts become clearer I-mprove reasoning O-ffers more effective communication N-egative symptoms reduced S-low psychomotor activity Pharmacokinetics (typical) Chlorpromazine enters body thru the mouth Metabolized in the liver Accumulate in fatty tissue Chlorpromazine binds with plasma proteins (only fraction crosses blood-brain barrier) Released slowly (even after months of therapy had stopped)-reason why effect still continues; noncompliance may occur Chlorpromazine-enters CNS rapidly tranquilizing effect occurs within 60 minutes (oral) and 10 minutes (IM) Excreted in the urine (traces of drug metabolites present even months after therapy had stopped) SOME IMPORTANT NOTES: Chlorpromazine –more potent in elderly because of decreased protein-binding action Oral routes are preferred more Liquid forms preferred for non-compliant patients (should be diluted to counteract unpleasant taste)-problem of cheeking Parenteral preferred for noncompliance and out patients (Haloperidol decanoate or fluphenazine decanoate)- 1-2X A MONTH A client with schizophrenia, undifferentiated type, is receiving a typical antipsychotic/ neuroleptic. The nurse should be alert for extrapyramidal signs and symptoms, which include: A. shuffling gait, tremors, and restlessness B. nausea, vomiting, and muscular cramps C. drowsiness, disorientation, and slurred speech D. tachycardia, urinary retention, and constipation A client with schizophrenia is given antipsychotic drugs. The nurse is aware that of all the extrapyramidal effects associated with these drugs, the one causing the most concern would be: A. akathisia B. tardive dyskinesia C. parkinsonian syndrome D. an acute dystonic reaction Side effects - PNS Anticholinergic effects –blocking acetylcholine Hypotension-blocking of alpha1 receptors which prevents constriction of blood vessels in upright position Side Effects- CNS (PANTD) Pseudoparkinsonism Akathisia NMS-neuroleptic malignant syndrome Tardive dyskinesia Dystonia- torticollis, oculogyric crisis and opisthotonus PARKINSONISM Motor retardation or akinesia characterized by mask-like appearance, rigidity, tremors, “pill- rolling”, salivation Generally occurs after 1st week of treatment or before second month Administer anticholinergic agent, anti- parkinson medication (Akineton) AKATHISIA Constant state of movement, characterized by restlessness, difficulty sitting still, or strong urges to move about Generally occurs two weeks after treatment begins Rule out anxiety or agitation before administration of an anticholinergic agent DYSTONIA DYSTONIA Painful and frightening spasms of tongue, throat, face, jaw, eyes, neck, or back muscles T-torticollis O-oculogyric crisis O-opisthotonus Anticholinergic drugs Stay with the patient TARDIVE DYSKINESIA 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 20-25% of patients taking antipsychotics for over two years No treatment except discontinuation of the antipsychotic agent NMS A potentially fatal syndrome May occur anytime during therapy Seen during the initiation of therapy, change of therapy, After a dosage increase or when a combination of meds is used. Early sign: rigidity or mental status changes catatonia, tachycardia, tachypnea, labile blood pressure, dysphagia, diaphoresis, incontinence, rigidity, myoclonus, tremors, high grade fevers Discontinue antipsychotic agent. Have cardiopulmonary support available; administer skeletal muscle relaxant(e.g. dantrolene) or central acting dopamine agonist (e.g. bromocriptine) Summary of Side Effects of Neuroleptics B -blurred vision P-pseudoparkinsonism U -urinary retention A-agranulocytosis C-constipation N-NMS O-orthostasis D-dystonia A-anxiety A -akathisia N-nausea T-tardive dyskinesia SOME NOTES: Use in elderly – lower doses due to decreased hepatic metabolism capacity Use in pregnant women- readily passes placental barrier and may cause EPSs to the fetus If used with CNS depressants, can cause profound CNS depression Clozapine (Clozaril) Possible mechanisms of agranulocytosis: 1. clozapine metabolite, desmethylclozapine, may have direct cytotoxic effect on the bone marrow cells 2. Release of granulocyte-stimulating factor maybe suppressed by clozapine, resulting in hematologic imbalance 3. Clozapine may induce antibody formations that are toxic to peripheral blood neutrophils and their committed precursors Antidepressants and Anti- manic agents  TRICYCLIC ANTIDEPRESSANTS  A client has been taking imipramine (Tofranil) for his depression for 2 days. His sister asks the nurse, “Why is he still so depressed?” Which of the following responses by the nurse would be most appropriate? a. “Your brother is experiencing a very serious depression.” b. “I’ll be sure to convey your concern to his physician.” c. “It takes 2 to 4 weeks for the drug to reach its full effect.” d. “Perhaps we’ll need to change his medication.” TCAs: ANTIDEPRESSANTS (TCA’s) =15 “MAMA, DEDE NA ACO, PARA TATABA DIVA?” (GENERIC) M-MAPTROPTILINE (LUDIOMIL) M- MIRTAZAPINE (REMERON) D- DOXEPIN (SINEQUAN) D-DESIPRAMINE (NORPRAMIN) N- NORTRIPTYLINE (AVENTYL, PAMELOR) A-AMOXAPINE (ASENDIN) C- CLOMIPRAMINE (ANAFRANIL)…best for OCD P-PROTRIPTYLINE (VIVACTIL) T-TRAZODONE (DESYRYL) T-TRIMIPRAMINE (SURMONTIL) B- BUPROPION (WELLBUTRIN) D-DULOXETINE(CYMBALTA) I-IMIPRAMINE (TOFRANIL) V-VENLAFAXINE (EFFEXOR) … (SNRI) A- AMITRIPTYLINE (ELAVIL)  BRAND NAMES)- “LURE, SINO AVEN, ASEN ANA VIDES? SUR, WELL, CYMTO paEFFEX ni ELA”  SSRIs Flouxetine (Proxac) Fluvoxamine (Luvox) Paroxetine (Paxil) Sertraline (Zoloft) MAOIs Moclobemide (Manerix)- reversible Phenelzine (Nardil) Tranylcypromine (Parnate) Isocarboxacid (Marplan) ANTIMANIC Carbamazepine (Tegretol) Lithium Carbonate (Eskalith) Valproic Acid (Depakene) TCAs: Contains three hydrocarbon rings Inhibits neurotransmitter reuptake (NE and SE) Intended Effects S-sedative/hypnotic T-treatment of chronic pain D-decreased symptoms of depression T-treatment of anxiety associated with depression, alcoholism, neurotic disorders I-improved appetite-weight gain T-treatment of panic attacks and phobic attacks SIDE OR ADVERSE EFFECTS W- Weight gain A-Agitation I-Insomnia S-Sedation A-Arrhythmias C-Confusion (esp.elderly) O-Orthostatic hypotension A-Anticholinergic effects Pharmacological Effects (TCA) Serum level of amines in the depressed person is low TCA blocks reuptake of amines Greater neurotransmitter availability Prolonged stimulating action Alleviates symptoms ABSORPTION Absorbed well in the GIT Metabolized in the liver Binds with plasma proteins Peak plasma concentrations reached at 2-4 hours Inhibits amine reuptake Side Effects PNS side Effects- orthostatic hypotension CNS side effects: A-nticholinergic effects D-isorientation D-elusions S-edation C-onfusion A-gitations S-eizure threshold lowered H-allucinations Lower doses or OD for elderly, alcoholics, history of hepatitis Connection to suicide: depressed people are also suicidal but antidepressants may cause the “lifting” in these patients which may warrant close monitoring/suicide precaution Drug interactions with TCAs Drug Effect of interaction Cimetidine Increased TCA serum levels MAOIs Hyperpyrexia, excitability, muscular rigidity, convulsions, fatal hypertensive crisis, mania Barbiturates,carbama Decreased TCA effect zepine, phenytoin Antipsychotics Increased EPSEs, sedation, hypotension, risk of seizures, anticholinergic effect Alcohol, Increased sedation anticonvulsants, benzodiazepines  Teaching patients: OTC avoided-to prevent drug interactions Two-four weeks –before full therapeutic effects occur Eye pain-report immediately (narrow angle glaucoma) Adjustment- to medication can lessen some side effects Slow discontinuation- to avoid nausea, headache and malaise Individual TCAs AMITRIPTYLINE(ELAVIL) -prescribed often but not for the elderly -Highly anticholinergic -one of the most sedating and cardiotoxic antidepressants -parenteral form and in fixed dose combination with antipsychotics Perphenazine (Triavil)  AMOXIPINE (ASENDIN) -metabolite of g drug loxapine -blocks dopamine receptors -potential for tardive dyskinesia; -not for elderly  DESIPRAMIN (NORPRAMIN) -metabolite of imipramine -Good choice for elderly patients who are sensitive to anticholinergic side effects -minor anticholinergic effects -activating antidepressant (for apathetic, lethargic, hypersomic) -less sedating -therapeutic to panic attacks and dysthymia  DOXEPIN (SINEQUAN) -potentiates serotonin; sedating, has anticholinergic activity; high antianxiety effects -Few cardiovascular effects but can have orthostatic hypotension and weight gain -may have antiulcer properties  IMIPRAMINE (TOFRANIL) -oldest TCA; more effective -for children enuresis -first-line drug in the treatment of panic disorder -the standard by which newer antidepressants are measured -care with children due to its cardiovascular effects  MAPROTILINE (LUDIOMIL) -potentiates norepinephrine -with anticholinergic effects; sedating -a strong antianxiety effect -no cardiovascular risk  NORTRIPTYLINE (AVENTYL, PAMELOR) -for people with history of unfavorable responses to antidepressants -for elderly; less orthostatic hypotension -sedating; for agitated and insomnia  PROTRIPTYLINE (VIVACTIL) -potentiates norepinephrine much more than serotonin -greater incidence of tachycardia, cardiovascular problems and orthostatic hypertensions; has anticholinergic effects  BUPROPION (WELLBUTRIN) -inhibits dopamine reuptake -minimal orthostatic hypotension, cardiovascular problems, anticholinergic effects and daytime sedation -activating antidepressant -contraindicated for patients with seizure disorders ( lowers seizure threshold) -can cause weight loss -effective replacement for SSRIs -reduces craving for cigarettes  NEFAZODONE (SERZONE) -first line agent for depression -inhibits serotonin and norepinephrine reuptake; blocks serotonin receptors -does not cause insomnia, sexual dysfunction, nervousness  TRAZODONE(DESYREL) -Potentiates serotonin not norepinephrine -almost no anticholinergic effects -few cardiac effects -sedating; for insomnia -absorption is increased right after a light meal -adverse reaction is priapism (prolonged penile erection); nurse should stop the medication and notify the prescriber  MIRTAZAPINE (REMERON) -for major depression only -blocks alpha2 receptors which increases norepinephrine and serotonin by utilizing the presynaptic feedback system (signals need for more of these neurotransmitters  TRAZODONE(DESYREL) -Potentiates serotonin not norepinephrine -almost no anticholinergic effects -few cardiac effects -sedating; for insomnia -absorption is increased right after a light meal -adverse reaction is priapism (prolonged penile erection); nurse should stop the medication and notify the prescriber  VENLAFAXINE (EFFEXOR) -SNRI, norepinephrine reuptake inhibitor -few anticholinergic, antihistaminic, or antiadrenergic side effects -does not exaggerate the effects of alcohol -maybe effective in treating SSRI-induced sexual dysfunction, panic disorders and OCD SSRI First choice for depression Fewer anticholinergic, cardiovascular and sedating effects OD dosing Tolerated in the elderly SIDE EFFECTS: DOWN D2 D-decreased libido O-orgasm decreased W-weight loss N-nervousness,, D-diarrhea D-dizziness, TOXICITY: VITMN V- vomiting I-irritability T-tremor M-myoclonus (twitching of a muscle or group of muscles) N-nausea INTERACTIONS DRUG EFFECT OF INTERACTION Irreversible MAOIs AVOID! Can be fatal Lithium Increased lithium levels Antipsychotics Increased EPSEs Benzodiazepines Increased benzo half-life TCA Increased TCA serum levels- toxicity Carbamazepine, Increased anti-convulsant phenytoin serum levels SEROTONIN SYNDROME Potentially fatal with SSRI + MAOI Hyperreflexia, hyperthermia, myoclonus, NMS Should: 1. Be aware that a period of 14 days is required between stopping a MAOI and starting a SSRI 2. Be aware of a period of 5 weeks is required between stopping an SSRI Flouxetine (Prozac) and starting a MAOI 3. Be aware that MAOIs and clomipramine (Anafranil) should not be given concomintantly INDIVIDUAL SSRIs 1.FLOUXETINE (PROZAC) -first SSRI; treatment for bulimia 2.SERTRALINE (ZOLOFT) -potent inhibitor of serotonin reuptake than flouxetine -inhibit ejaculation in men and orgasm in women; orgasmic ability returns after 2-3 days after drug cessation 3.PAROXETINE(PAXIL) -most potent SSRI -Treatment of panic attacks; prevention of depression relapse -side effect: nausea -delays or inhibits orgasm 4.FLUOVOXAMINE(LUVOX) -for OCD A client who is receiving MAO inhibitor is going home on a weekend pass. Considering this drug, the nurse plan to caution the client to avoid: A. pork, spinach, and fresh oysters B. milk, peanut butter, and meat tenderizers C. cheese, beer, and products with chocolate D. orange drinks, fresh apples, and ice cream MAOI Administered to hospitalized patients Derivative of isoniazid, iproniazid (Anti-TB) Blocks monoamine oxidase Effect from 10 days to 2 weeks Causes decreased heart rate, decreased vasoconstriction and hypotension (slowed release of norepinephrine in PNS) Inhibits MAO in the liver, leads to elevated levels of other drugs metabolized in the liver by MAO Side effects: cardiovascular and anticholinergic effects Blood counts and liver function tests before therapy TYRAMINE INTERACTION Amino acid, tyramine (precursor of dopamine, epinephrine and norepinephrine) Foods: (principle: foods aged, left to spoil) A-alcohol/avocado B-bananas C-chicken liver/caffeinated coffee/colas/ chocolate D-dairy products/dried fish S-salami/sausage/soy sauce T-tea  Symptoms of hypertensive crisis:,,, D-Dilation of pupils C-Chest tightness H-high blood pressure P-Palpitation D-Diaphoresis, I-Increased heart rate, S-Stiff neck H-Headache (throbbing, radiating ) TEACHING PATIENTS: Hypertensive crisis symptoms must be reported immediately OTC drugs (some) must be avoided Tyramine-rich foods, avoid except for reversible MAOI SSRI + MAOI is fatal, so avoid Ten days-4 weeks before full therapeutic effects occur Driving avoided due to drowsiness IRREVERSIBLE MAOIs PHENELZINE (NARDIL) -most effective MAOI, most sedative -deterrent to cocaine abuse and for panic attacks TRANYLCYPROMINE (PARNATE) -for severe reactive depression -most stimulating -contraindicated to elderly REVERSIBLE MAOI MOCLOBEMIDE (MANERIX) -inhibition lasts only 24 hours -taken after meals to reduce tyramine-related responses  ANTIMANIC LITHIUM (ESKALITH) CARBAMAZEPINE(TEGRETOL) VALPROIC ACID (DEPAKENE) LAMOTIGRINE (LAMICTAL)  Assessment of which o the following clients would lead to the nurse to expect the physician to order an adjustment in lithium dosage. a. A client who continues work as a computer programmer. b. A client who attends college classes. c. A client who is now able to care for his or her children. d. A client who is beginning training for a tennis team. LITHIUM  LITHIUM Not much significant than sodium Treatment of manic depression Absorbed in the GIT, peak blood levels of 1-3 hours Not metabolized, excreted by the kidneys unchanged Absorption of lithium and sodium are closely linked If dietary sodium intake increases, plasma lithium levels will drop (lithium excreted more rapidly) If NA in the diet decreases, lithium levels increase 7-10 days for therapeutic effects Maintenance level: 0.5-1.5 mEq/L (900-1200mg/day) Side effects that subside: nausea, dry mouth, thirst, mild hand tremor, weight gain, insomnia, light-headedness Side effects which will not subside: vomiting, severe tremors, sedation, muscle weakness, vertigo Contraindication: persons with cardiovascular diseases Interactions: diuretics-decreases lithium excretion, low-salt diet increases lithium levels TEACHING PATIENTS: T-try not to instill anxiety by preparing patients for expected side effects R-report immediately side effects which will not subside (vomiting, severe tremors, sedation, muscle weakness, vertigo) E-Elevate feet to relieve ankle edema M-maintain normal fluid balance of at least 3 liters of water per day O-On side effects that subside, discuss them with the patient (nausea, dry mouth, thirst, mild hand tremor, weight gain, insomnia, light-headedness) R-Reduce nausea by taking lithium with meals S- Sodium intake must be maintained CARBAMAZEPINE Antimanic, anticonvulsant Side effects: drowsiness ,dizziness, unsteadiness, upset stomach vomiting, headache, anxiety, memory problems, diarrhea, constipation, heartburn dry mouth, back pain Can cause agranulocytosis and aplastic anemia VALPROIC ACID ANTIMANIC, ANTICONVULSANT Side effects: drowsiness, Dizziness, headache, diarrhea, constipation, heartburn, changes in appetite, weight changes, back pain , unusual bruising or bleeding, tiny purple spots on the skin Can cause liver dysfunction, hepatic failure, blood dyscrasias including thrombocytopenia Teaching Patients  Other medications should be prescribed to avoid adverse drug interactions  Report bruising, can be thrombocytopenia  Swallowed, not chewed, cut or crushed to avoid irritation  Avoid machineries, driving due to drowsiness  Liver and renal functions tests, CBCs to prevent serious complications  Take with food to avoid nausea ANTIANXIETY ANTIANXIETY Minor tranquilizers, anxiolytics Benzodiazepines (major class) Generally depressing effect  hyperalertness, stress, environmental scanning (end of continuum-anxiety) Antianxiety given Metabolized by liver Crosses blood-brain barrier easily (lipid-soluble) Potentiates GABA Depresses CNS, limbic system,thalamus, hypothalamus,reticular activating system Relaxed feeling or care-free feeling (one end of continuum) *this makes it frequently abused by users SIDE EFFECTS Drowsiness, fatigue, decreased coordination Slowing of reflexes Less frequent: confusion, headache, depression Occasional constipation, double vision, hypotension, incontinence, urinary retention Triple problem: 1. Tolerance 2. Withdrawal –agitation, tremor, irritability, insomnia, vomiting, sweating, convulsions 3. dependence  TEACHING PATIENTS: B-Benzodiazepines are not for minor stresses of everyday life U-Use of other benzo must be avoided if hypersensitive to one benzo S-Should not be stopped abruptly to prevent withdrawal symptoms P-Patient should be assisted during ambulation I-Instruct patient not to drive until tolerance develops R-Report to physician if systole is 20mmHg on standing and stop the drug O-Other CNS depressants and ALCOHOL should be avoided-potentiates effects of benzo N-Nausea can be avoided by taking drug with meals E-Effect of BUSPAR (nonbenzo) is 2-4 weeks Used only in a short time (1-2 weeks) Tolerance (after 7 days) and dependence (after 1 month) Liver function test Monitor for side effects. Avoid machines, activities needing concentration Z tract if given parenterally Avoid mixing with alcohol, antacids Don’t stop abruptly but gradually for 2-6 weeks Avoid caffeine Avoid grapefruit juice (inhibits enzyme metabolism) OX SER, DI VA, LORA AT CHLORDI LI, AL XA CHLORA TRAN? CLO KLO talaga cla!  DIAZEPAM (VALIUM) -Antianxiety, preoperatively used to relieve presurgery jitters -adjunct to endoscopic procedures -relief of symptomatic alcohol withdrawal ALPRAZOLAM (XANAX) - GAD, adjustment disorders, anxiety associated with depression, panic disorder CHLORDIAZEPOXIDE (LIBRIUM) -acute alcohol withdrawal, anxiety disorders CLONAZEPAM (KLONOPIN) -most often as anticonvulsant -Panic disorder CLORAZEPATE (TRANXENE) -Anxiety and acute alcohol withdrawal -adjunct in the treatment of partial seizures LORAZEPAM (ATIVAN) -anxiety disorders OXAZEPAM (SERAX) -Suitable for elderly and persons with liver functions Other anxiolytics Buspirone (Buspar) Flurazepam (Dalmane) Hydroxyzine (Atarax, Vistaril) Meprobamate (Miltown) Midazolam (Versed) Temazepan (Restoril) Q&A SITUATION: You are the medication nurse for 1 week on a psychiatric unit. You have a busy week. Respond to the questions for each example given: 1. Your client has been prescribed Fluphenazine (Prolixin). The client has never taken this medication. What type of medication is this? Identify four side effects that the client might experience. A- Antipsychotic. Orthostatic hypotension, dizziness, drowsiness, constipation. EPSs can also be experienced. 2. M.H. is taking Procyclidine (Kemadrin). Why would this medication be prescribed? A- M.H. must be taking an antipsychotic medication. Kemadrin is used to prevent or moderate EPS symptoms caused by antipsychotics. 3. A.P. has been prescribed Lithium soon after her admission. She is very angry and aggressive. What is wrong with the statement, “The Lithium will soon stop that behavior?” A- Lithium does not work quickly, and the client may need an anipsychotic medication in addition to the Lithium in the initial stages of treatment. 4. A.P. begins to experience hand tremors, polyuria, confusion and ataxia. What is happening to A. P.? What do you need to do initially? A- A.P. is experiencing toxicity to Lithium. You need to hold the next dose and call her primary care provider. 5. A. P. will need to be taught about her diet. What will you teach Her? A- lithium should be taken with food. The client needs a balanced diet with adequate fluid and sodium intake. 6.B. F. has been taking Oxazepam (Serax). He has found that he needs a higher dose to get its desired effect. What has happened to B.F.? A- B.F. has developed a tolerance to the drug and may have developed a dependency on the drug. 7. A.K. is taking Alprazolam (Xanax). She says, “I have a fear of addiction, but I don’t mind taking this medication because I know I can’t get addicted to it.” How would you respond to this statement? A- You can be dependent on antianxiety medications, such as Xanax. These drugs need to be used as prescribed with medical supervision. 8. You are assessing a new client who has schizophrenia. You note that he has facial grimaces, tongue thrusting, and makes a smacking sound. What is the client’s problem? What is a cause of this problem? A- The client is experiencing Tardive Dyskinesia (TD). This is a serious side effect from taking antipsychotic medications. It’s irreversible. 9.Elderly clients will need higher doses of medications in order to obtain positive results from psychotropic medications. Why is this a false statement? A-Elderly clients need lower doses because their kidney and liver function is not usually able to tolerate high doses. 10. A client on the unit has been prescribed isocarboxacid (marplan). What intervention is critical for this client? A- the client requires a special diet and education about it. The diet must be free of tyramine. 1. The nurse is planning discharge teaching with a client taking CLozapine( Clorazil). Which of the following is essential to include? A. Caution client not to be outdoors in the sunshine without protective clothing. B. Remind the client to go to the lab to have blood drawn foe a WBC count. C. Instruct the client about dietary restriction. D. Give the client a chart to record a daily pulse rate. 2. The nurse is caring for a client who has been taking Fluphenazine (Prolixin) for 2 days. the client suddenly cries out, his neck twists to one side and his eyes appear to roll back in the sockets. The nurse finds the following prn medications ordered for the client. Which one should the nurse administer? A. Benztropine (Cogentin) 2 mg p.o. BID prn B. Fluphenazine (Prolixin) 2 mg p.o. TID prn C. Haloperidol 5mg IM prn extreme agitation D. Diphenhydramine (Benadryl) 25mg IM prn 3. One of the side effects of antipsychotic drug is Pseudoparkinsonism. To combat this effect, which of the following drugs must be ordered? A. Diazepam(Valium) B. Clozapine (Corazil) C. Biperiden(Akineton) D. Amitryptaline(Elavil) 4. A nurse is caring for a client who will be taking tranylcypromine (Parnate). The client has been taking sertraline (Zoloft) for the past several weeks. Before the administration of Parnate, which of the following would be essential to ensure for this client? A.Teach the client about the purpose of the medication B.Allow 2 weeks for the Zoloft to exert its effects C.Discontinue Zoloft for 2 weeks before starting Parnate D.Limit alcohol to two glasses of wine daily  5. A client with a chronic mental illness has worked as a hotel maid for the past 3 years. She tells the nurse she is thinking of quitting her job because “voices on television are talking about me.” What would be the nurse’s initial action? A.Obtain information about the client’s medication compliance. B.Remind the client that hearing voices is a symptom of her illness with which she can cope. C.Check with the client’s employer about her work performance. D.Arrange for the client to be admitted to a psychiatric hospital for a short stay. 6.Thirty minutes after administering fluphenazine (Prolixin) to a client, the nurse notices the client’s jaw is rigid, the tongue is thick, the client is drooling, and speech is slurred. There are a number of prn orders in the client’s chart. The nurse should administer A. Haloperidol (Haldol), 2 mg IM B. Diazepam (Valium), 10 mg PO C. Benztropine (Cogentin), 2 mg IM D. Trihexyphenidyl (Artane), 1 mg PO 7. During the manic phase of bipolar I disorder, a client’s lithium level is 0.15 mEq/L. the client dresses flamboyantly, acts provocatively, and has seriously impaired judgment. What is the nurse’s first priority when planning this client’s care? A. administer lithium carbonate I.M. B. observe the client’s behavior closely in the milieu C. Begin aversion therapy to extinguish undesirable behaviors D. initiate suicide precautions because the client’s judgment is impaired  8. Three days ago, a client with chronic schizophrenia received 20 mg of Haldol decanoate by I.M. injection. Now the client has muscle contractions that contort the neck. The client is demonstrating which extrapyramidal reaction? A. dystonia B. akinesia C. akathisia D. tardive dyskinesia