NCM 106 Pharmacology Learning Module PDF

University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM...

University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Learning Module in NCM 106 PHARMACOLOGY Prepared by: John Ian L. Lamasan, M.A.N., R.N. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM NCM 106: PHARMACOLOGY MODULE 4 DRUGS AFFECTING IN THE BODY SYSTEM Module Overview This module is designed for nursing students to have a comprehensive introduction to the concepts, principles of Pharmacology and to Integrate knowledge of physical, social, natural and health sciences and humanities in nursing pharmacology Module Outcomes At the end of the module the learner should be able to: 1. Provide appropriate health education related to drug therapy. 2. Evaluate compliance and response of client to the medications prescribed. 3. Use available clinical evidence that can ensure safe medication administration. 4. Document client’s condition/response/ outcomes related to drug therapy. 5. Manage resources (human, physical, financial, time) efficiently and effectively in safe drug administration. Use appropriate communication/ interpersonal techniques/strategies to ensure a working relationship with the client and/or support system in medication administration. Ensure intra-agency, inter-agency, multidisciplinary and sectoral collaboration in medication administration. Assume personal responsibility to keep abreast with current trends in nursing pharmacology Exemplify love for country in the service of the Filipinos. Discuss various technological advances in ensuring safe medication administration Manifest professionalism and excellence in planning for safe medication practice. Module Content: Central Nervous System (Autonomic and Peripheral Nervous System) Anxiolytic and hypnotic agents Antidepressant agents Psychotherapeutic Antiepileptic agents Antiparkinsonism agents Muscle relaxants Narcotics and anti-migraine drugs General and local anesthetics Neuromuscular blocking agents Autonomic Nervous System Adrenergic agents Adrenergic blocking agents Cholinergic agents Cholinergic blocking agents A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Course Content: ANXIOLYTICS AND HYPNOTIC AGENTS ANXIOLYTICS  Also known antianxiety drugs.  They are primarily used to treat anxiety and insomnia. Primary anxiety is not caused by a medical condition or by drug use. Secondary anxiety is related to selected drug use or medical or psychiatric disorders. CLINICAL MANIFESTATIONS OF ANXIETY  Dyspnea  Choking sensation  Chest pain  Heart palpitations  Dizziness  Faintness  Sweating  Trembling and shaking  Fear of losing control NON PHARMACOLOGIC MEASURES  Using of relaxation technique  Psychotherapy  Support groups PHARMACOLOGIC MEASURES BENZODIAZEPINES  Used as anticonvulsants, sedative-hypnotics, preoperative drugs, substance abuse withdrawal agents, and anxiolytics.  Used mainly for severe or prolonged anxiety.  Example includes chlordiazepoxide (Librium), diazepam (Valium), clorazepate dipotassium (Tranxene), lorazepam (Ativan), and alprazolam (Xanax). Generic Name Route & Indication & Side Effects & Pregnancy (Brand Name) Dosage Mechanism of Action Adverse Reactions Category Lorazepam Adults:  To control anxiety and to Side Effects D (Ativan) PO treat status epilepticus Drowsiness, dizziness, 2-6 mg/d;  For preoperative sedation weakness, confusion, blurred max: 10 mg/d  For substance withdrawal vision, nausea, vomiting, anorexia, restlessness, Older adults: Potentiate gamma- hallucinations, anterograde PO aminobutyric (GABA) amnesia, sleep-related 1-2 mg/d; effects by binding to behaviors max: 10 mg/d specific benzodiazepine receptors and inhibiting Adverse Reactions GABA neurotransmission Hypertension, hypotension, bradycardia, respiratory depression A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Contraindications Hypersensitivity, CNS depression, shock, coma, narrow-angle glaucoma, seizures, alcohol intoxication, liver impairment, pregnancy, lactation NURSING RESPONSIBILITIES  Observe patient for side effects of anxiolytics. Recognize that drug tolerance and physical and psychological dependency can occur with most anxiolytics.  Recognize that anxiolytic dosages should be lower for older adults, children, and debilitated persons than for middle-aged adults.  Monitor vital signs, especially blood pressure and pulse; orthostatic hypotension may occur.  Encourage family to be supportive of patient. Health Teachings  Encourage patient to rise slowly from sitting to standing position to avoid dizziness from orthostatic hypotension.  Advise patient not to drive a motor vehicle or operate dangerous equipment when taking anxiolytics, because sedation is a common side effect.  Warn patient not to consume alcohol or CNS depressants such as narcotics while taking an anxiolytic.  Teach patient ways to control excess stress and anxiety (relaxation techniques, long walks).  Inform patient that effective response may take 1 to 2 weeks.  Encourage patient to follow drug regimen and not to abruptly stop taking the drug after prolonged use because withdrawal symptoms can occur. Drug dose is usually tapered when drug is discontinued. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM SEDATIVE-HYPNOTICS  For treatment of sleep disorders. Short-acting hypnotics are useful in achieving sleep, because they allow the patient to awaken early in the morning without experiencing lingering side effects. Intermediate-acting hypnotics are useful for sustaining sleep; however, after using one the patient may experience residual drowsiness, or hangover, in the morning. NONPHARMACOLOGIC METHODS TO PROMOTE SLEEP  Arise at a specific hour in the morning.  Take few or no daytime naps.  Avoid drinks that contain caffeine and alcohol 6 hours before bedtime. Also avoid smoking nicotine 6 hours before bedtime.  Avoid heavy meals or strenuous exercise before bedtime.  Take a warm bath, listen to quiet music, or perform other soothing activities before bed.  Decrease exposure to loud noises.  Avoid drinking copious amounts of fluids before sleep.  Drink warm milk before bedtime. PHARMACOLOGIC MEASURES BARBITURATES Long-acting barbiturates  Used to control seizures in epilepsy.  phenobarbital and mephobarbital Intermediate-acting barbiturates  Used as sleep sustainers for maintaining long periods of sleep.  Butabarbital (Butisol) Short-acting barbiturates  Used primarily for sedation preoperatively.  secobarbital (Seconal) and pentobarbital (Nembutal) Ultrashort-acting barbiturates  Used as a general anesthetic.  thiopental sodium (Pentothal) NONBENZODIAZEPINES It is used for short term treatment (less than 10 days) of insomnia. Generic Name Route & Indication & Side Effects & Pregnancy (Brand Name) Dosage Mechanism of Action Adverse Reactions Category Zolpidem Adult To treat insomnia Side Effects C Tartrate PO Drowsiness, lethargy, headache, (Ambien) 5-10 mg h.s.; Mode of Action: hot flashes, hangover (residual max: 10 mg/d CNS depression, sedation), irritability, dizziness, neurotransmitter ataxia, visual disturbances, Older adults inhibition anxiety, mental depression, PO nausea and vomiting, erectile 5 mg h.s.; max: dysfunction 5-10 mg/d Adverse Reactions A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Tolerance, psychological or physical dependence; sleep- related behaviors, hypotension, angioedema, dysrhythmias, suicidal ideation Contraindications Hypersensitivity to benzodiazepine, respiratory depression, lactation NURSING RESPONSIBILITIES: HYPNOTICS  Monitor vital signs. Check for signs of respiratory depression (slow, irregular breathing patterns).  Use bed alarm for older adults or patients receiving nonbenzodiazepines for the first time. Confusion may occur, and injury may result.  Observe patient for side effects of nonbenzodiazepines (e.g., hangover [residual sedation], lightheadedness, dizziness, confusion). HEALTH TEACHINGS  Teach patient to use nonpharmacologic ways to induce sleep (taking a warm bath, listening to music, drinking warm fluids such as milk, avoiding drinks with caffeine after dinner).  Encourage patient to avoid alcohol, antidepressant, antipsychotic, and narcotic drugs while taking nonbenzodiazepines. Severe respiratory depression may occur when these drugs are combined.  Advise patient to take nonbenzodiazepine before bed time. Alprazolam takes effect within 15 to 30 minutes.  Suggest that patient urinate before taking nonbenzodiazepine to prevent sleep disruption.  Encourage patient to check with health care provider about OTC sleeping aids.  Drowsiness may result from taking these drugs, so caution while driving is advised.  Advise patient to report adverse reactions such as hangover to health care provider. Drug selection or dosage may need to be changed if hangover occurs. MELATONIN AGONISTS Ramelteon (Rozerem) is in the newest category of sedative/hypnotics.  This drug acts by selectively targeting melatonin receptors to regulate circadian rhythm in the treatment of insomnia.  It has not been shown to decrease REM sleep.  Adverse effects of ramelteon include drowsiness, dizziness, fatigue, headache, nausea, and suicidal ideation.  It is also used as an antianxiety drug. Activity 1 Read and Analyse Instruction: 1. Read and analyse the case scene. 2. Briefly write your answer in the comment section. Case Scene: JZ, a 72-year-old woman, has difficulty staying asleep. She asks the nurse whether she should take a hypnotic. Before JZ takes any sleep aid or hypnotic, what nursing assessments should be made? A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM ANTIDEPRESSANT AGENTS AND MOOD STABILIZERS ANTIDEPRESSANTS  Used for depressive episodes that are accompanied by feelings of hopelessness and helplessness.  They can be prescribed for 1 month to 12 months or perhaps longer. DEPRESSION is characterized primarily by mood changes and loss of interest in normal activities. CONTRIBUTING CAUSES OF DEPRESSION  Genetic predisposition  Social and environmental factors  Biologic conditions. SIGNS OF MAJOR DEPRESSION  Loss of interest in most activities  Depressed mood  Weight loss or gain  Insomnia or hypersomnia  Loss of energy  Fatigue  Feelings of despair  Decreased ability to think or concentrate  Suicidal thoughts THREE TYPES OF DEPRESSION Reactive depression usually has a sudden onset after a precipitating event (e.g., depression resulting from a loss, such as death of a loved one). The patient knows why he or she is depressed and may call this “the blues.” Usually this type of depression lasts for months. A benzodiazepine agent may be prescribed. Major depression is characterized by loss of interest in work and home, inability to complete tasks, and deep depression (dysphoria). Antidepressants have been effective in treating major depression. Primary is not related to other health problems. Secondary to a health problem (e.g., physical or psychiatric disorder or drug use). Bipolar affective disorder involves swings between two moods, the manic (euphoric) and the depressive (dysphoria). Lithium (Lithobid) was originally the drug of choice for treating this type of disorder. Other mood stabilizers, such as carbamazepine (Tegretol), valproic acid or divalproex (Depakote, Valproate), and lamotrigine (Lamictal) are also currently first-line drugs of choice for bipolar disorder. ANTIDEPRESSANT AGENTS 1. Tricyclic Antidepressants (TCAs), or Tricyclics 2. Selective Serotonin Reuptake Inhibitors (SSRIs) 3. Serotonin Norepinephrine Reuptake Inhibitors (SNRIs) 4. Atypical Antidepressants that affect various neurotransmitters 5. Monoamine Oxidase Inhibitors (MAOIs). TRICYCLIC ANTIDEPRESSANTS (TCAs)  Block the uptake of the neurotransmitters norepinephrine and serotonin in the brain.  Clinical response of TCAs occurs after 2 to 4 weeks of drug therapy.  Elevate mood, increase interest in daily living and activity, and decrease insomnia. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM LIST OF TRICYCLIC ANTIDEPRESSANTS o amitriptyline (Elavil) o clomipramine HCl (Anafranil) o desipramine HCl (Norpramin) o doxepin (Silenor) o imipramine (Tofranil) o nortriptyline (Pamelor/ Aventyl) o protriptyline (Vivactil) o trimipramine (Surmontil) SIDE EFFECTS o Orthostatic hypotension o Sedation o Anticholinergic effects o Allergic reactions (skin rash, pruritus, and petechiae) and sexual dysfunction (impotence and amenorrhea). ADVERSE REACTIONS o Blood dyscrasias (leukopenia, thrombocytopenia, and agranulocytosis) requiring close monitoring of blood cell counts. o Extrapyramidal symptoms (EPS) o Neuroleptic malignant syndrome (NMS) o Seizure o Cardiotoxicity, such as dysrhythmias that may result from high doses of the drug. Note: The therapeutic serum range is 100 to 200 ng/mL. WARNING! Alcohol, hypnotics, sedatives, and barbiturates potentiate central nervous system (CNS) depression when taken with TCAs. Concurrent use of MAOIs with amitriptyline may lead to cardiovascular instability and toxic psychosis. Antithyroid medications taken with amitriptyline may increase the risk of dysrhythmias. SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs)  Block the reuptake of serotonin into the nerve terminal of the CNS, thereby enhancing its transmission at the serotonergic synapse.  Do not block the uptake of dopamine or norepinephrine, and they do not block cholinergic and alpha1-adrenergic receptors.  Commonly used to treat depression than are TCAs.  They have fewer side effects than TCAs LIST OF SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs) o fluoxetine (Prozac) o fluvoxamine (Luvox) o sertraline (Zoloft) o paroxetine (Paxil) o citalopram (Celexa) o escitalopram (Lexapro) SIDE EFFECTS o Dry mouth o Blurred vision o Insomnia o Headache o Nervousness A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM o Tremors o Anorexia o Nausea o Diarrhea o Sexual Dysfunction ADVERSE REACTIONS o Seizures o Hyponatremia o Dehydration o Bleeding o Osteopenia o Suicidal ideation Note: Many SSRIs have an interaction with grapefruit juice that can lead to possible toxicity. It is recommended that daily intake be limited to 8 ounces of grapefruit juice or one half of a grapefruit. SEROTONIN NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs)  Inhibit the reuptake of serotonin and norepinephrine, increasing availability in the synapse.  Used for major depression  Other approved uses are for generalized anxiety disorder and social anxiety disorder. LIST OF SEROTONIN NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs) o duloxetine (Cymbalta) o desvenlafaxine (Pristiq) o venlafaxine (Effexor) SIDE EFFECTS o Drowsiness o Dizziness o Insomnia o Headache o Euphoria o Amnesia o Blurred vision o Photosensitivity o Ejaculation dysfunction ADVERSE EFFECTS o Hyponatremia o Bleeding o Hypertension o Angioedema o Blood dyscrasias o Suicidal ideation o StevensJohnson syndrome ATYPICAL ANTIDEPRESSANTS  Also known as Second-generation antidepressants  Used for major depression, reactive depression, and anxiety.  They affect one or two of the three neurotransmitters: serotonin, norepinephrine, and dopamine. Note: Atypical antidepressants should not be taken with MAOIs and should not be used within 14 days after discontinuing MAOIs. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM LIST OF ATYPICAL ANTIDEPRESSANTS o amitriptyline (Elavil) o clomipramine (Anafranil) o desipramine (Norpramin) o doxepin (Sinequan) o imipramine (Tofranil) o nortriptyline (Aventyl) o protriptyline (Vivactil) o trimipramine (Surmontil) SIDE EFFECTS o Drowsiness o Dizziness o Orthostatic hypotension o Dry mouth o Constipation o Urinary retention ADVERSE REACTION o Suicidal ideation MONOAMINE OXIDASE INHIBITORS  The enzyme monoamine oxidase (MAO) inactivates norepinephrine, dopamine, epinephrine, and serotonin. By inhibiting MAO, the levels of these neurotransmitters rise.  There are two forms of MAO enzyme: MAO-A and MAO-B. These enzymes are found primarily in the liver and brain. MAO-A inactivates dopamine in the brain, whereas MAO-B inactivates norepinephrine and serotonin.  The MAOIs are nonselective, inhibiting both MAO-A and MAO-B. LIST OF MONOAMINE OXIDASE INHIBITORS o tranylcypromine sulfate (Parnate) o isocarboxazid (Marplan) o selegiline HCl (Emsam, Eldepryl) o phenelzine sulfate (Nardil) SIDE EFFECTS o CNS stimulation (agitation, restlessness, and insomnia) o Orthostatic hypotension o Anticholinergic effects. Note: Any drugs that are CNS stimulants or sympathomimetics (e.g., vasoconstrictors and cold medications containing phenylephrine and pseudoephedrine) can cause a hypertensive crisis when taken with an MAOI. Foods that contain tyramine (cheese [cheddar, Swiss, bleu], cream yogurt, coffee, chocolate, bananas,raisins,Italian green beans, liver, pickled foods, sausage, soy sauce, yeast, beer, and red wines) have sympathomimetic-like effects and can cause a hypertensive crisis. NURSING RESPONSIBILITIES: ANTIDEPRESSANTS  Observe patient for signs and symptoms of depression: mood changes, insomnia, apathy, or lack of interest in activities.  Monitor patient’s vital signs. Orthostatic hypotension is common. Check for anticholinergic-like symptoms: dry mouth, increased heart rate, urinary retention, or constipation. Check weight two to three times per week.  Monitor patient for suicidal tendencies when marked depression is present. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM  Observe patient for seizures when patient is taking an anticonvulsant; antidepressants lower the seizure threshold. The anticonvulsant dose might need to be increased.  Monitor for drug-drug and food-drug interactions. Sympathomimetic-like drugs and foods containing tyramine may cause a hypertensive crisis if taken with MAOIs.  Check patient for extremely high blood pressure when taking MAOIs.  Provide patient with a list of foods to avoid when taking MAOIs to avoid hypertensive crisis. These foods include cheese, red wine, beer, liver, bananas, yogurt, and sausage. Patient Teaching HEALTH TEACHINGS  Teach patient to take the medication as prescribed. Compliance is important.  Inform patient that full effectiveness of drug may not be evident until 1 to 2 weeks after start of therapy.  Encourage patient to keep medical appointments.  Caution patient not to consume alcohol or any CNS depressants because of their addictive effect.  Inform patient that many herbal products interact with antidepressants, especially MAOIs and SSRIs. Herbs may need to be discontinued, or the antidepressant drug dosage may need to be modified (see Herbal Alerts 28-1 and 28-2).  Warn patient not to drive or be involved in potentially dangerous mechanical activity until stabilization of drug dose has been established.  Advise patient not to abruptly stop taking the drug. Drug dose should be gradually decreased by health care provider.  Encourage patient who is planning pregnancy to consult with health care provider about possible teratogenic effects of the drug on the fetus.  Take with food if gastrointestinal (GI) distress occurs.  Advise patient that antidepressants may be taken at bedtime to decrease dangers from the sedative effect. Have patient check with health care provider. Transient side effects include nausea, drowsiness, headaches, and nervousness. MOOD STABILIZERS  Used to treat bipolar affective disorder.  Lithium (Lithobid), carbamazepine (Tegretol), valproic acid or divalproex (Depakote, Valproate), and lamotrigine (Lamictal) are currently first-line drugs for bipolar disorder. Note: Lithium has a narrow therapeutic serum range: 0.5 to 1.5 mEq/L. Serum lithium levels greater than 1.5 to 2 mEq/L are toxic. Generic Name Route & Indication & Side Effects & Pregnancy (Brand Name) Dosage Mechanism of Action Adverse Reactions Category Lithium Adult: To treat bipolar Side Effects D (Eskalith) PO psychosis, manic Headache, memory impairment, (Lithane) initially 600 mg episodes blurred vision, metallic taste, (Lithonate) t.i.d.; dental caries, lethargy, (Lithobid) maint: 300 mg Mode of Action: drowsiness, dizziness, tremors, (Carbolith) t.i.d./q.i.d.; Alteration of ion slurred speech, dry mouth, (Lithizine) max: 2.4 g/d transport in muscle and anorexia, vomiting, diarrhea, nerve cells; increased polyuria, dehydration, Child: receptor sensitivity to hypotension, abdominal pain, PO serotonin. muscle weakness, restlessness 15 to 20 mg/kg/d in 3-4 Adverse Reactions divided doses Urinary and fecal incontinence, hyperglycemia, hyponatremia, Therapeutic proteinurea, polyurea, A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM drug range: leukocytosis, nephrotoxicity Life- 0.5-1.5 mEq/L threatening: Cardiac dysrhythmias, seizures, cardiac arrest, serotonin syndrome, neuroleptic malignant syndrome Contraindications Liver and renal disease, pregnancy, lactation, severe cardiovascular disease, severe dehydration, hyponatremia, children 6 y therapies. PO It is used to control 10 mg/kg/d in divided grand mal and partial doses; seizures and a max: 35 mg/kg/d combination of these seizures. Child: 6-12 y s also used for 100 mg b.i.d.; psychiatric disorders max: 1g/d (e.g., bipolar disease), trigeminal neuralgia Therapeutic serum range: (as an analgesic), and 5-12 mcg/mL alcohol withdrawal VALPROATE valproate, PO For psychomotor, D valproic acid, 10-15 mg/kg/d in divided myoclonic, absence, divalproex Na doses; and tonic-clonic (Depakote) Increase 5-10 mg/kg/d seizures. Also weekly until seizures approved for bipolar controlled; disorder and migraine max: 60 mg/kg/d prophylaxis A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Therapeutic serum range: 50-100 mcg/mL NURSING RESPONSIBILITIES  Monitor serum drug levels of anticonvulsant to determine therapeutic range (10 to 20 mcg/mL).  Encourage patient’s compliance to medication regimen.  Monitor patient’s CBC levels for early detection of blood dyscrasias.  Use seizure precautions (environmental protection from sharp objects, such as table corners) for patients at risk for seizures.  Determine whether patient is receiving adequate nutrients; phenytoin may cause anorexia, nausea, and vomiting.  Advise female patients who are taking oral contraceptives and anticonvulsants to use an additional contraceptive method. HEALTH TEACHING  Teach patient to shake suspension form thoroughly before use to adequately mix medication and assure accurate dosage.  Advise patient not to drive or perform other hazardous activities when initiating anticonvulsant therapy as drowsiness may occur.  Counsel female patients contemplating pregnancy to consult with health care provider, because phenytoin and valproic acid may have a teratogenic effect.  Monitor serum phenytoin levels closely during pregnancy, because seizures tend to become more frequent due to increased metabolic rates.  Warn patient to avoid alcohol and other CNS depressants, because they can cause an added depressive effect on the body.  Explain to patient that certain herbs can interact with an anticonvulsant drug and dose adjustment may be required.  Encourage patient to obtain medical alert identification card, medical alert bracelet, or tag that indicates health diagnosis and drug regimen.  Teach patient not to abruptly stop drug therapy, but rather to withdraw the prescribed drug gradually under medical supervision to prevent seizure rebound (recurrence of seizures) and status epilepticus (continuous seizure state).  Counsel patient about the need for preventive dental checkups.  Warn patient to take prescribed anticonvulsant, get laboratory tests as ordered, and keep follow-up visits with health care provider.  Teach patient not to self-medicate with over-the-counter (OTC) drugs without first consulting health care provider.  Advise patient with diabetes to monitor serum glucose levels more closely than usual because phenytoin may inhibit insulin release, causing an increase in glucose level.  Inform patient of the existence of national, state, and local associations that provide resources, current information, and support for persons with epilepsy.  Coach patient to take anticonvulsant at the same time every day with food or milk.  Tell patient that urine may be a harmless pinkish red or reddish brown.  Advise patient to maintain good oral hygiene and to use a soft toothbrush to prevent gum irritation and bleeding.  Teach patient to report symptoms of sore throat, bruising, and nosebleeds, which may indicate a blood dyscrasia.  Encourage patient to inform health care provider of adverse reactions such as gingivitis, nystagmus, slurred speech, rash, and dizziness. Stevens-Johnson syndrome begins with a rash. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Activity 4 Read and Analyse Instruction: 1. Read and analyse the case scene. 2. Briefly write your answer in the comment section. Case Scene: SS, a 26-year-old woman, takes phenytoin 100 mg t.i.d. to control grand mal seizures. The nurse checks SS’s serum phenytoin level. What are the indications of an abnormal serum level? What appropriate actions should be taken? A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM ANTIPARKINSONISM AGENTS Parkinsonism (Parkinson’s disease)  A chronic neurologic disorder that affects the extrapyramidal motor tract (which controls posture, balance, and locomotion).  It is caused by an imbalance of the neurotransmitters dopamine (DA) and acetylcholine (ACh).  It is marked by degeneration of neurons of the extrapyramidal motor tract. The reason for the degeneration of neurons is unknown. PATHOPHYSIOLOGY OF PARKINSONISM There are two neurotransmitters within neurons of the striatum of the brain: dopamine, an inhibitory neurotransmitter, and acetylcholine, an excitatory neurotransmitter. Dopamine is released from the dopaminergic neurons; acetylcholine is released from the cholinergic neurons. Dopamine normally maintains control of acetylcholine and inhibits its excitatory response. In parkinsonism, there is an unexplained degeneration of the dopaminergic neurons, and an imbalance between dopamine and acetylcholine occurs. With less dopamine production, the excitatory response of acetylcholine exceeds the inhibitory response of dopamine. An excessive amount of acetylcholine stimulates neurons that release GABA. With increased stimulation of GABA, the symptomatic movement disorders of parkinsonism occur. Three symptoms were described by Parkinson: 1. Involuntary tremors of the limbs 2. Rigidity of muscles 3. Slowness of movement (bradykinesia) Pseudoparkinsonism frequently occurs as an adverse reaction to antipsychotic drugs, especially the phenothiazines. NONPHARMACOLOGIC MEASURES  Patient teaching  Exercise ( Therapeutic exercise program )  Nutrition ( Balanced diet with fiber and fluids )  Group support Drugs used to treat parkinsonism reduce the symptoms or replace the dopamine deficit. These drugs fall into five categories: 1. Anticholinergics- block cholinergic receptors 2. Dopamine replacements- stimulate dopamine receptors 3. Dopamine agonists- stimulate dopamine receptors 4. MAO-B inhibitors- inhibit the monoamine oxidase-B (MAO-B) enzyme that interferes with dopamine 5. COMT inhibitors- inhibit the catechol O-methyltransferase enzyme that inactivates dopamine. ANTICHOLINERGIC DRUGS  They reduce the rigidity and some of the tremors characteristic of parkinsonism but have minimal effect on bradykinesia.  These are parasympatholytics that inhibit the release of acetylcholine.  They are still used to treat drug-induced parkinsonism, or pseudoparkinsonism, a side effect of the antipsychotic drug group phenothiazines.  Examples of anticholinergics used for parkinsonism include trihexyphenidyl (Artane), benztropine (Cogentin), and biperiden (Akineton). A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Side Effects:  Dry mouth  Blurred vision  Drowsiness  Muscle weakness  Constipation Contraindications:  Patients with glaucoma  GI obstruction  Severe ulcerative colitis  Prostatic hypertrophy  Myasthenia gravis NURSING RESPONSIBILITIES  Monitor vital signs, urine output, and bowel sounds. Increased pulse rate, urinary retention, and constipation are side effects of anticholinergics.  Observe for involuntary movements. HEALTH TEACHINGS  Advise patient to avoid alcohol, cigarettes, caffeine, and aspirin to decrease gastric acidity.  Encourage patient to relieve dry mouth with hard candy, ice chips, or sugarless chewing gum. Anticholinergics decrease salivation.  Suggest that patient use sunglasses in direct sunlight because of possible photophobia.  Advise patient to void before taking the drug to minimize urinary retention.  Counsel patient who takes an anticholinergic for control of symptoms of parkinsonism to have routine eye examinations because patients who have glaucoma should not take anticholinergics.  Encourage patient to ingest foods high in fiber and increase fluid intake to prevent constipation. DOPAMINERGICS  levodopa was effective in diminishing symptoms of Parkinson’s disease and increasing mobility, because the blood-brain barrier admits levodopa but not dopamine.  The enzyme dopa decarboxylase converts levodopa to dopamine in the brain, but this enzyme is also found in the peripheral nervous system and allows 99% of levodopa to be converted to dopamine before it reaches the brain. Therefore only about 1% of levodopa taken is available to be converted to dopamine once it reaches the brain, and large doses are needed to achieve a pharmacologic response.  carbidopa, was developed to inhibit the enzyme dopa decarboxylase. By inhibiting the enzyme in the peripheral nervous system, more levodopa reaches the brain. The carbidopa is combined with levodopa in a ratio of 1 part carbidopa to 10 parts levodopa.  Carbidopa-Levodopa (Sinemet)  To treat parkinsonism; to relieve tremors and rigidity Mode of Action: Transmission of levodopa to brain cells for conversion to dopamine; carbidopa blocks the conversion of levodopa to dopamine in the intestine and peripheral tissues Advantages of combining levodopa with carbidopa:  More dopamine reaches the basal ganglia.  Smaller doses of levodopa are required to achieve the desired effect. Disadvantage of the carbidopa-levodopa combination is that with more available levodopa, more side effects may be noted. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Side Effects:  Anorexia  Nausea  Vomiting  Dysphagia  Fatigue  Dizziness  Headache  Dry mouth  Bitter taste  Twitching  Blurred vision  Insomnia  Dark urine Adverse Reactions:  Involuntary movements  Palpitations  Orthostatic hypotension  Urinary retention  Priapism  Psychosis  Severe depression with suicidal ideation  Hallucinations Contraindications:  Narrow-angle glaucoma  Severe cardiac, renal, hepatic disease  Suspicious skin lesions (activates malignant melanoma) NURSING RESPONSIBILITIES  Monitor patient’s vital signs and electrocardiogram. Orthostatic hypotension may occur during early use of levodopa and bromocriptine. Instruct patient to rise slowly to avoid faintness.  Observe for weakness, dizziness, or syncope, which are symptoms of orthostatic hypotension.  Administer carbidopa-levodopa (Sinemet) with lowprotein foods. High-protein diets interfere with drug transport to the CNS.  Observe for symptoms of parkinsonism. HEALTH TEACHINGS  Urge patient not to abruptly discontinue the medication. Rebound parkinsonism (increased symptoms of parkinsonism) can occur.  Inform patient that urine may be discolored and will darken with exposure to air. Perspiration also may be dark. Explain that both are harmless but clothes may be stained.  Advise patient to avoid chewing or crushing extended release tablets.  Encourage patient to report side effects and symptoms of dyskinesia. Explain to patient that it may take weeks or months before symptoms are controlled.  Suggest to patient that taking levodopa with food may decrease GI upset, but food will slow the drug absorption rate.  Urge patient who takes high doses of selegiline to avoid foods high in tyramine (e.g., aged cheese, red wine, cream, yogurt, chocolate, bananas, raisins) to prevent hypertensive crisis. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM DOPAMINE AGONISTS  Stimulate the dopamine receptors.  amantadine hydrochloride (Symmetrel) is an antiviral drug that acts on the dopamine receptors. It may be taken alone or in combination with carbidopa-levodopa or an anticholinergic drug. Initially, amantadine produces improvement in symptoms of parkinsonism in approximately two thirds of patients, but this improvement is usually not sustained, because drug tolerance develops. Amantadine can also be used to treat drug induced parkinsonism.  bromocriptine mesylate (Parlodel) acts directly on dopamine receptors in the central nervous system (CNS), cardiovascularsystem,andgastrointestinal(GI)tract.Bromocriptine is more effective than amantadine and the anticholinergics; however, it is not as effective as carbidopa-levodopa in alleviating parkinsonism symptoms. Patients who do not tolerate carbidopa-levodopa are frequently given bromocriptine. Side Effects:  Hypotension  Lightheadedness  Syncope  Nausea  Fatigue  Somnolence MAO-B INHIBITORS  The enzyme monoamine oxidase-B (MAO-B) causes catabolism (breakdown) of dopamine.  Selegiline inhibits MAO-B, thus prolonging the action of levodopa. It may be ordered for newly diagnosed patients with parkinsonism. The use of selegiline could delay carbidopa-levodopa therapy by 1 year. It decreases “on-off” fluctuations.  Rasagiline (Azilect) is an MAO-B inhibitor used for the treatment of parkinsonism.  Large doses of selegiline may inhibit MAO-A, an enzyme that promotes metabolism of tyramine in the GI tract. If they are not metabolized by MAO-A, ingestion of foods high in tyramine (aged cheese, red wine, and bananas) can cause a hypertensive crisis. Severe adverse drug interactions can occur between selegiline and various tricyclic antidepressants (TCA) or selective serotonin reuptake inhibitors (SSRIs). COMT INHIBITORS  The enzyme catechol O-methyltransferase (COMT) inactivates dopamine. When taken with a levodopa preparation, COMT inhibitors increase the amount of levodopa concentration in the brain.  Tolcapone (Tasmar) was the first COMT inhibitor taken with levodopa for advanced parkinsonism.  entacapone (Comtan) Contraindications:  Tolcapone (Tasmar) may cause severe liver damage. Patients with liver dysfunction should not take this drug.  Entacapone (Comtan) is not known to affect liver function. Side Effects:  entacapone, the urine can be dark yellow to orange  tolcapone, the urine can be bright yellow. Adverse Reactions:  Both tolcapone and entacapone can intensify the adverse reactions of levodopa (e.g., hallucinations, orthostatic hypotension, constipation, dizziness) because these drugs prolong the effect of levodopa. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM COMPARISON OF DRUGS USED TO TREAT PARKINSON’S DISEASE DRUG PURPOSE Anticholinergics; First group of drugs used to treat Parkinson’s disease before levodopa and dopamine Antiparkinson agonists were introduced. Useful in decreasing tremors related to Parkinson’s disease. The major use of these agents currently is to treat drug-induced parkinsonism. Treatment starts with low dosages, and then dose is gradually increased. Older adults are more susceptible to the many side effects of anticholinergics. Patients with memory loss or dementia should not be on anticholinergic therapy Dopaminergics Decreases symptoms of parkinsonism. Carbidopa, a decarboxylase inhibitor, permits carbidopa-levodopa more levodopa to reach the striatum nerve terminals (where levodopa is converted to dopamine). With the use of carbidopa, less levodopa is needed. Dopamine Agonists amantadine First used as an antiviral drug for influenza A. Decreases symptoms of parkinsonism. Can be used for early treatment of Parkinson’s disease, which could delay the necessity of levodopa. Is effective in treating drug-induced parkinsonism, and has fewer side effects than anticholinergics. bromocriptine A D2-dopamine receptor agonist. Can be used for early treatment of Parkinson’s disease. With increasing motor symptoms, can be given with levodopa therapy. pramipexole D2- and D3-dopamine receptor agonists. Can be used in combination with levodopa. (Mirapex), Fewer side effects than older dopamine agonists. ropinirole HCl (Requip) MAO-B Inhibitors selegiline HCl Inhibits catabolic enzymes of dopamine. Extends action of dopamine. Can be used for (Eldepryl) early treatment of Parkinson’s disease. If given with levodopa, dosage of levodopa is usually decreased. rasagiline (Azilect) Inhibits breakdown of dopamine at synapses in the brain. Allows neurons to reabsorb more dopamine for use later. COMT Inhibitors Inhibits COMT enzyme, increasing concentration of levodopa. Used in combination entacapone with levodopa-carbidopa (Sinemet). With COMT inhibitors, smaller dose of levodopa (Comtan), is needed. tolcapone (Tasmar) ALZHEIMER’S DISEASE  It is an incurable dementia illness characterized by chronic, progressive neurodegenerative conditions with marked cognitive dysfunction.  Onset usually occurs between 45 and 65 years of age. Theories related to the changes that cause Alzheimer’s disease:  Degeneration of the cholinergic neuron and deficiency in acetylcholine  Neuritic plaques that form mainly outside of the neurons and in the cerebral cortex.  Apolipoprotein E4 (apo E4) that promotes formation of neuritic plaques, which binds beta- amyloid in the plaques  Beta-amyloid protein accumulation in high levels that may contribute to neuronal injury  Presence of neurofibrillary tangles with twists inside the neurons A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Histologic changes in Alzheimer’s disease A. Healthy neuron. B. Neuron affected by Alzheimer’s disease showing characteristic neuritic plaques and cellular neurofibrillary tangles. Factors thought to influence the occurrence of Alzheimer’s disease are genetic predisposition, virus, infection, or inflammation that attacks brain cells, as well as nutritional, environmental, and immunologic. ACETYLCHOLINESTERASE INHIBITORS/CHOLINESTERASE INHIBITORS  AChE is an enzyme responsible for breaking down ACh and is also known as cholinesterase.  tacrine (Cognex); donepezil (Aricept); and rivastigmine (Exelon), drug that permits more acetylcholine in the neuron receptors.  Rivastigmine has effective penetration into the CNS; thus, cholinergic transmission is increased.  These AChE inhibitors increase cognitive function for patients with mild to moderate Alzheimer’s disease. A reversible AChE inhibitor used to treat mild to moderate Alzheimer’s disease is galantamine (Razadyne). Side Effects:  Anorexia  Nausea  Vomiting  Diarrhea  Constipation  Abdominal pain  Gastrointestinal bleeding  Dizziness  Depression  Peripheral edema  Dry mouth  Dehydration  Restless legs syndrome  Nystagmus Adverse Reactions:  Seizures  Bradycardia  Orthostatic hypotension  Cataracts  Myocardial infarction  Heart failure Contraindications:  Liver and renal diseases  Urinary tract obstruction  Orthostatic hypotension  Bradycardia A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM NURSING RESPONSIBILITIESS  Maintain consistency in care.  Assist patient in ambulation and activity.  Monitor for side effects related to continuous use of AChE inhibitors.  Record vital signs periodically. Note signs of bradycardia and hypotension.  Observe patient’s behavioral changes, and record improvement or decline Patient HEALTH TEACHINGS  Explain to patient and family the purpose for prescribed drug therapy.  Clarify time for drug dosing and schedule for increasing drug dosing to family member responsible for patient’s medications.  Teach family member about safety techniques (e.g., removing obstacles from patient’s path so that patient can avoid injury when wandering).  Inform family member of available support groups such as the Alzheimer’s Disease and Related Disorders Association.  Inform patient and family member that patient should rise slowly to avoid dizziness and loss of balance.  Monitor routine liver function tests, as hepatotoxicity is an adverse effect.  Inform family member about foods that may be prepared for patient’s consumption and tolerance. Activity 5 Read and Analyse Instruction: 1. Read and analyse the case scene. 2. Briefly write your answer in the comment section of the discussion board. Case Scene: TR, a 79-year-old man, was diagnosed with Parkinson’s disease 10 years ago. During his early treatment, he took selegiline. The drug dosage was increased to alleviate symptoms. 1. How does selegiline alleviate symptoms of parkinsonism? 2. What dietary changes should be made during the time TR takes selegiline? A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM MUSCLE RELAXANTS  Relieve muscular spasms and pain associated with traumatic injuries and spasticity from chronic debilitating disorders (e.g., MS, stroke [cerebrovascular accident], cerebral palsy, head and spinal cord injuries).  Spasticity results from increased muscle tone from hyperexcitable neurons caused by increased stimulation from the cerebral neurons or lack of inhibition in the spinal cord or at the skeletal muscles.  The centrally acting muscle relaxants depress neuron activity in the spinal cord or brain or enhance neuronal inhibition on the skeletal muscles. CENTRALLY ACTING MUSCLE RELAXANTS  The mechanism of action is not fully known.  They are used in cases of spasticity to suppress hyperactive reflex and for muscle spasms that do not respond to antiinflammatory agents, physical therapy, or other forms of therapy.  cyclobenzaprine (Flexeril), carisoprodol (Soma), chlorzoxazone (Parafon forte DSC), methocarbamol (Robaxin), metaxalone (Skelaxin) and orphenadrine citrate (Norflex). MUSCLE RELAXANTS DRUGS USES Anxiolytics To relieve muscle spasms associated with paraplegia and cerebral diazepam (Valium) palsy Spasticity (Centrally Acting) For muscle spasms caused by MS and spinal cord injury. Overdose baclofen (Lioresal), may cause CNS depression. tizanidine (Zanaflex) Spasticity (Direct Acting) For chronic neurologic disorders causing spasms: spinal cord dantrolene sodium (Dantrium) injuries, stroke, MS. Centrally Acting Muscle Relaxants For relaxation of skeletal muscles carisoprodol (Soma), chlorzoxazone (Parafon forte DSC), methocarbamol (Robaxin), metaxalone (Skelaxin) orphenadrine citrate (Norflex). Depolarizing Muscle Relaxants For surgical skeletal muscle relaxation. Also used in endoscopy (Adjunct to Anesthesia) and intubation succinylcholine (Anectine) Nondepolarizing Muscle Relaxants Used in surgery for relaxation of skeletal muscle (Adjunct to Anesthesia) pancuronium bromide (Pavulon), vecuronium (Norcuron) Side Effects:  Anticholinergic effects (blurred vision, constipation, dry mouth, tachycardia, urinary retention)  Drowsiness  Dizziness  Headache  Fever  Abdominal pain  Vomiting  Diarrhea  Flatulence  Erectile dysfunction A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Adverse Reactions:  Allergic reactions  Angioedema  Myocardial infarction  Seizures  Ileus Contraindications:  Acute myocardial infarction  AV blocks, bundle-branch block  Cardiac arrhythmias  Heart failure  Hyperthyroidism  Paralytic ileus  Concurrent use of monoamine oxidase inhibitors or within 14 days after discontinuation NURSING RESPONSIBILITIES  Monitor serum liver enzyme levels of patients taking dantrolene and carisoprodol. Report elevated levels of liver enzymes such as alkaline phosphatase (ALP), alanine aminotransferase (ALT), and gamma-glutamyl transferase (GGT).  Record vital signs. Report abnormal results.  Observe for CNS side effects (e.g., dizziness). HEALTH TEACHING  Teach patient that the muscle relaxant should not be abruptly stopped. Drug should be tapered over 1 week to avoid rebound spasms.  Advise patient not to drive or operate dangerous machinery when taking muscle relaxants. These drugs have a sedative effect and can cause drowsiness.  Inform patient that most of the centrally acting muscle relaxants for acute spasms are usually taken for no longer than 3 weeks.  Teach patient to avoid alcohol and CNS depressants. If muscle relaxants are taken with these drugs, CNS depression may be intensified.  Advise patient that these drugs must be used cautiously for pregnant or nursing patients. Check with health care provider.  Encourage patient to report side effects of the muscle relaxant: nausea, vomiting, dizziness, fainting, headache, and diplopia. Dizziness and fainting are most likely caused by orthostatic (postural) hypotension.  Advise patient to take muscle relaxants with food to decrease gastrointestinal upset. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM NONOPIOID AND OPIOID ANALGESICS Pain is an unpleasant sensory and emotional experience related to tissue injury. Due to the subjective nature of pain, the nurse must be knowledgeable and skillful in the assessment and measurement of pain to achieve optimal pain management. Nociceptors (sensory pain receptors) are activated by noxious stimuli (mechanical, thermal, and chemical) in peripheral tissues. When tissue damage occurs, injured cells release chemical mediators that affect the exposed nerve endings of the nociceptors. Pain that originates from tissue injury is nociceptor pain, which includes somatic (structural tissues: bones, muscles) and visceral (organ) pain. Neuropathic pain is an unusual sensory disturbance often involving neural supersensitivity. This pain is due to injury or disease of the peripheral or central nervous system (CNS). Patients with neuropathic pain usually complains of burning, tingling, or electrical shocks in the affected area, often triggered by light touch. PATHOPHYSIOLOGY OF PAIN According to the gate theory proposed by Melzack and Wall in 1965, tissue injury activates nociceptors and causes the release of chemical mediators such as substance P, prostaglandins, bradykinin, histamine, serotonin, acetylcholine, glutamate, adenosine triphosphate, leukotrienes, and potassium. These substances initiate an action potential along a sensory nerve fiber and sensitize pain receptors. Nociceptive action potentials are transmitted via afferent nerve fibers. One type of pain fiber that primarily transmits impulses from the periphery is the A delta (δ) fiber. Because A δ pain fibers are wrapped in a myelin sheath, they transmit impulses rapidly in acute pain. The C fiber is a type of pain fiber that is small and unmyelinated, and because C fibers are unmyelinated, they transmit impulses slowly. C fibers are more often associated with chronic, dull pain. TYPES OF PAIN AND ITS DRUG TREATMENT TYPE OF PAIN DEFINITION DRUG TREATMENT Acute Pain occurs suddenly and Mild pain: responds to treatment; can result Scheduled nonopioid (acetaminophen, NSAIDs q6h) from trauma, tissue injury, Moderate pain: inflammation, or surgery Scheduled combination of nonopioid and opioid (oxycodone 5 mg and acetaminophen 325 mg q4h) Severe pain: Scheduled potent opioid (morphine 15 mg q4h) Chronic Pain persists for greater than 6 Nonopioid drugs are suggested. months and is difficult to treat or Opioids, if used, should meet these criteria: control Oral or transdermal Long duration of action Include adjunct therapy Cause minimal respiratory depression Cancer Pain from pressure on nerves and NSAIDs and opioid drugs administered PO, organs, blockage to blood supply, transdermal, IM, IV, or PCA or metastasis to bone Somatic Pain of skeletal muscle, Nonopioids: NSAIDs; also act as antiinflammatories ligaments, and joints and muscle relaxants Superficial Pain from surface areas such as Mild pain: Nonopioid skin and mucous membranes Moderate pain: Combination of opioid and nonopioid analgesic drug A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Vascular Pain from vascular or perivascular Nonopioid drugs tissues contributing to headaches or migraines Visceral Pain from smooth muscle and Opioid drugs organs NONOPIOID ANALGESICS  Nonopioid analgesics (aspirin, acetaminophen, ibuprofen, naproxen) are less potent than opioid analgesics.  They are used to treat mild to moderate pain.  They are usually purchased over-the-counter (OTC), but COX-2 inhibitors require a prescription. Nonopioids are effective for the dull, throbbing pain of headaches, dysmenorrhea (menstrual pain), inflammation, minor abrasions, muscular aches and pain, and mild to moderate arthritis.  Most analgesics also have an antipyretic effect and will lower an elevated body temperature.  Some, such as aspirin, have antiinflammatory and antiplatelet effects as well. NONSTEROIDAL ANTIINFLAMMATORY DRUGS  All NSAIDs have an analgesic effect as well as an antipyretic and antiinflammatory action. NSAIDs such as aspirin (ASA), ibuprofen (Motrin, Advil), and naproxen (Aleve) can be purchased as OTC drugs.  Aspirin, a salicylate NSAID, is the oldest nonopioid analgesic drug still in use. In addition to its analgesic, antipyretic, and antiinflammatory properties, aspirin decreases platelet aggregation (clotting).  Aspirin and other NSAIDs relieve pain by inhibiting biosynthesis of prostaglandin by different forms of the enzyme cyclooxygenase (COX). Inhibition of COX-2 decreases inflammation and pain, but inhibition of COX-1 decreases protection of the stomach lining. There are seven groups of NSAIDs: 1. Salicylates 2. Para-chlorobenzoic acid derivatives, or indoles 3. Phenylacetic acids 4. Propionic acid derivatives 5. Fenamates 6. Oxicams 7. Selective COX-2 inhibitors SALICYLATES  Aspirin comes from the family of salicylates derived from salicylic acid.  Aspirin is also called acetylsalicylic acid (ASA) after the acetyl group used in the composition of aspirin.  Aspirin is a prostaglandin inhibitor that decreases the inflammatory process.  It is also considered an antiplatelet drug for patients with cardiac or cerebrovascular disorders; aspirin decreases platelet aggregation, and thus blood clotting is decreased.  Aspirin should not be taken with other NSAIDs because it decreases the blood level and effectiveness of NSAIDs.  aspirin (ASA, Bayer, Ecotrin), diflunisal (Dolobid), olsalazine sodium (Dipentum), and sulfasalazine (Azulfidine) A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Side Effects  Anorexia  Nausea  Vomiting  Diarrhea  Dizziness  Confusion  Hearing loss  Heartburn  Rash  Abdominal pain  Drowsiness Adverse Reactions  Tinnitus  Urticaria  Ulceration  GI bleeding Contraindications  Hypersensitivity to salicylates or NSAIDs  Flu or virus symptoms in children  Anticoagulant therapy  GI bleeding  Bone marrow suppression  Third trimester of pregnancy NURSING RESPONSIBILITIES  Monitor serum salicylate (aspirin) level when patient takes high doses of aspirin for chronic conditions such as arthritis. Normal therapeutic range is 15 to 30 mg/ dL. Mild toxicity occurs at serum level of >30 mg/dL, and severe toxicity occurs at >50 mg/dL.  Observe patient for signs of bleeding such as dark (tarry) stools, bleeding gums, petechiae (round red spots), ecchymosis (excessive bruising), and purpura (large red spots) when patient takes high doses of aspirin. HEALTH TEACHINGS  Advise patient not to take aspirin with alcohol or with drugs that are highly protein-bound, such as the anticoagulant warfarin (Coumadin). Aspirin displaces drugs like warfarin from the protein-binding site, causing increased anticoagulant levels.  Suggest that patient inform the dentist before a dental visit if taking high doses of aspirin.  Instruct patient to discontinue aspirin 3 to 7 days before surgery to reduce risk of bleeding (with the health care provider’s approval).  Keep aspirin bottle out of reach of children.  Educate parent to call poison control center immediately if a child has taken a large or unknown amount of aspirin (or acetaminophen).  Warn patient not to administer aspirin for virus or flu symptoms in children. Reye’s syndrome (vomiting, lethargy, delirium, and coma) has been linked with aspirin and viral infections. Acetaminophen is usually prescribed for cold and flu symptoms.  Inform patient that aspirin tablets can cause GI distress.  Inform patient with dysmenorrhea to take acetaminophen instead of aspirin 2 days before and during the first 2 days of the menstrual period.  Direct patient to report side effects such as drowsiness, tinnitus (ringing in the ears), headaches, flushing, dizziness, GI symptoms (bleeding, heartburn), visual changes, and seizures. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM  Instruct patient to take aspirin (also ibuprofen) with food, at mealtime, or with plenty of fluids. EC aspirin helps prevent GI disturbance. PARA-CHLOROBENZOIC ACID  One of the first NSAIDs introduced was indomethacin (Indocin), a para-chlorobenzoic acid.  It is used for rheumatoid arthritis, gouty arthritis, and osteoarthritis and is a potent prostaglandin inhibitor.  Two other para-chlorobenzoic acid derivatives—sulindac (Clinoril) and tolmetin (Tolectin)—produce less severe adverse reactions than indomethacin.  This group of NSAIDs may cause sodium and water retention and increased blood pressure. PHENYLACETIC ACID DERIVATIVES  Diclofenac sodium (Voltaren-XR), a phenylacetic acid derivative.  Its analgesic and antiinflammatory effects are similar to those of aspirin, but it has minimal to no antipyretic effects.  It is indicated for rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis.  diclofenac sodium (Voltaren XR), etodolac (Lodine) and ketorolac tromethamine (Toradol) PROPIONIC ACID DERIVATIVES  They are relatively new group of NSAIDs.  These drugs are aspirin-like but have stronger effects and create less GI irritation.  Ibuprofen (Motrin) is the most widely used propionic acid NSAID, and it may be purchased OTC in lower doses (200 mg).  fenoprofen calcium (Nalfon), naproxen (Naprosyn), ketoprofen (Orudis), flurbiprofen (Ansaid), and oxaprozin (Daypro). Side Effects  Anorexia  Nausea  Vomiting  Diarrhea  Edema  Rash  Purpura  Tinnitus  Fatigue  Dizziness  Lightheadedness  Anxiety  Confusion  Fluid retention with edema Adverse Reactions  GI bleeding Contraindications  Severe renal or hepatic disease  Asthma  Peptic ulcer  Anticoagulant therapy A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM FENAMATES  Includes potent NSAIDs used for acute and chronic arthritic conditions.  Like most NSAIDs, gastric irritation is a common side effect of fenamates, and patients with a history of peptic ulcer should avoid taking this group of drugs.  Other side effects include edema, dizziness, tinnitus, and pruritus.  meclofenamate sodium monohydrate (Meclomen) and mefenamic acid (Ponstel) OXICAMS  Piroxicam (Feldene), an oxicam, is indicated for long-term arthritic conditions such as rheumatoid arthritis and osteoarthritis.  It too can cause gastric problems such as ulceration and epigastric distress, but the incidence is lower than for some other NSAIDs.  It is well tolerated, and its major advantage over other NSAIDs is its long half-life, which allows it to be taken only once daily.  Meloxicam (Mobic) SELECTIVE COX-2 INHIBITORS (SECOND-GENERATION NSAIDS)  Became available in the last several years to decrease inflammation and pain.  Most NSAIDs are nonselective inhibitors that inhibit COX-1 and COX-2.  By inhibiting COX-1, protection of the stomach lining is decreased and clotting time is also decreased, which may benefit the patient with cardiovascular or coronary artery disease (CAD).  Selective COX-2 inhibitors are drugs of choice for patients with severe arthritic conditions who need high doses of an antiinflammatory drug, because large doses of NSAIDs may cause peptic ulcer and gastric bleeding.  celecoxib (Celebrex) NURSING RESPONSIBILITES: NSAIDs  Observe patient for bleeding gums, petechiae, ecchy moses, or black (tarry) stools. Bleeding time can be prolonged when NSAIDs are taken, especially with a highly protein-bound drug such as warfarin (anticoagulant).  Report if patient has GI discomfort.Administer NSAIDs at mealtime or with food to prevent GI upset.  Monitor vital signs and check for peripheral edema, especially in the morning.  Do not give directions such as “take one blue pill” at a specified time. Instead, provide name and dosage of medication. HEALTH TEACHING  Inform patient not to take aspirin and acetaminophen with NSAIDs. Taking an NSAID with aspirin could cause GI upset and possible GI bleeding.  Inform patient to avoid alcohol when taking NSAIDs. GI upset or gastric ulcer may result.  Alert patient that many herbal products may interact with NSAIDs and could cause bleeding. Doses of NSAIDs and/or herbs may need to be modified to avoid possible bleeding occurrence.  Direct patient to inform the dentist or surgeon before a procedure when taking ibuprofen or other NSAIDs for a continuous period.  Warn female patients not to take NSAIDs 1 to 2 days before menstruation to avoid heavy menstrual flow. If discomfort occurs, acetaminophen is usually prescribed.  Advise pregnant patients to avoid NSAIDs. Congenital abnormalities may occur when NSAIDS are taken during early pregnancy, and excess bleeding might occur during delivery. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM  Inform patient that it may take several weeks to experience desired drug effect of some NSAIDs and disease modifying antirheumatic drugs (DMARDs).  Educate patient of the common side effects of NSAIDs. Nausea, vomiting, peripheral edema, GI upset, purpura or petechiae, or dizziness might occur. Report occurrences of side effects.  Advise patient to take NSAIDs with meals or snacks to reduce GI upset. ACETAMINOPHEN  The analgesic acetaminophen (paraaminophenol derivative) is a popular nonprescription drug for the relief of pain, discomfort, and fever in infants, children, adults, and older adults.  It is a nonopioid drug, but it is not an NSAID.  It does not have the antiinflammatory properties of aspirin, so it is not the drug of choice for any inflammatory process.  It constitutes 25% of all OTC drugs sold. Examples of OTC products that contain acetaminophen include Anacin; Excedrin; Midol: Maximum Strength Menstrual Formula; and Vicks: Cold & Flu Relief.  Acetaminophen (Tylenol) is an analgesic and antipyretic drug used for muscular aches and pains and for fever caused by viral infections.  It is a safe, effective drug when used at therapeutic doses. It causes little to no gastric distress and does not interfere with platelet aggregation.  An IV formulation was FDA approved in 2010 for treating pain and fever.  There is no link between acetaminophen and Reye’s syndrome, and it does not increase the potential for excessive bleeding if taken for dysmenorrhea, as do aspirin and NSAIDs. Side Effects  Anorexia  Nausea  Vomiting  Rash  Insomnia Adverse Reactions  Oliguria  Urticaria  Elevated liver enzymes Contraindications  Acetaminophen hypersensitivity  Severe hepatic or renal disease  Alcoholism NURSING RESPONSIBILITIES  Check liver enzyme tests such as alanine aminotransferase, alkaline phosphatase, gamma-glutamyl transferase, 5′ nucleotidase, and bilirubin for elevations in patients taking high doses or overdoses of acetaminophen. HEALTH TEACHINGS  Teach patient to keep acetaminophen out of children’s reach. Acetaminophen for children is available in flavored tablets and liquid. High doses can cause hepatotoxicity.  Advise patient not to self-medicate with acetaminophen longer than 10 days. Teach adult caregiver not to medicate child longer than 5 days without health care provider’s approval. A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM  Direct parent to call poison control center immediately if a child has taken a large or unknown amount of acetaminophen.  Teach patient to check acetaminophen dosage on package label of OTC drugs. Do not exceed the recommended dosage. Suggested safe adult acetaminophen dose is 2000 mg/d (2 g/day), not to exceed 4 g/day to avoid liver damage (see Prototype Drug Chart 26-1).  Encourage patient to report side effects. Overdosing can cause severe liver damage and death.  Inform patient that liver damage may occur with excess use of acetaminophen.  Check serum acetaminophen level if toxicity is suspected. Normal serum level is 5 to 20 mcg/mL; toxic level is >50 mcg/mL. Levels of >200 mcg/mL could indicate hepatotoxicity. The antidote for acetaminophen is acetylcysteine (Mucomyst). Dosage is based on serum acetaminophen level. OPIOID ANALGESICS  Also called opioid agonists.  They are prescribed for moderate and severe pain.  Morphine, a prototype opioid, is obtained from the sap of seed pods of the opium poppy plant.  Codeine is another drug obtained from opium.  They act mostly on the CNS. They act primarily by activating the µ receptors, while also exerting a weak activation of the kappa (κ) receptors. Analgesia, respiratory depression, euphoria, and sedation are effects of µ activation. Activation of κ receptors leads to analgesia and sedation, having no effect on respiratory depression and euphoria.  They not only suppress pain impulses but also respiration and coughing by acting on the respiratory and cough centers in the medulla of the brainstem.  Codeine is not as potent as morphine (1/15 to 1/20 as potent), but it also relieves mild to moderate pain and suppresses cough, which allows it also to be classified as an antitussive. Most opioids, with the exception of meperidine (Demerol), have an antitussive (cough suppression) effect.  Hydromorphone (Dilaudid) is a semisynthetic opioid similar to morphine. Side Effects  Anorexia  Nausea  Vomiting  Constipation  Drowsiness  Dizziness  Sedation  Confusion  Urinary retention  Rash  Blurred vision  Bradycardia  Flushing  Euphoria  Pruritus Adverse Reactions  Hypotension  Urticaria  Seizures  Ileus A Legacy of Excellent Education in Virtus et Scientia Email: [email protected] | Tel. No.: (033) 337-4841 to 44 | Fax No.: (033) 337-4403 jilamasan  University of San Agustin General Luna St., Iloilo City 5000, Philippines www.usa.edu.ph COLLEGE OF HEALTH AND ALLIED MEDICAL PROFESSIONS-NURSING PROGRAM Contraindication  Hypersensitivity  CNS or respiratory depression  tatus asthmaticus  Increased intracranial pressure  Shock  Alcoholism  Ileus  Hypovolemia NURSING RESPONSIBILITIES  Administer morphine before pain reaches its peak to maximize effectiveness of the drug.  Monitor vital signs at frequent intervals to detect respiratory changes. Respirations of < 10/ min can indicate respiratory distress.  Record patient’s urine output because urinary retention is a side effect of morphine. Urine output should be at least 600 mL/day.  Check bowel sounds for decreased peristalsis; constipation is a side effect of morphine. Dietary change or mild laxative might be needed.  Check for pupil changes and reaction. Pinpoint pupils can indicate morphine overdose.  Have naloxone (Narcan) available as an antidote to reverse respiratory depression if morphine overdose occurs.  Validate dose of morphine before its administration. Check older adults for alertness and orientation because confusion is a side effect of morphine. Use side rails, and take other safety precautions as necessary. HEALTH TEACHING  Encourage patient not to use alcohol or CNS depressants with any opioid analgesics such as morphine. Respiratory depression can result.  Suggest nonpharmacologic measures to relieve pain as patient recuperates from surgery. As recovery progresses, a nonopioid analgesic may be prescribed.  Alert patient that with continuous use, opioids such as morphine can