Antiparkinson Agents PDF

ANTIPARKINSONIS M AGENTS Created by: Group 2  WHAT IS ANTIPARKINSON AGENTS? Antiparkinson agents are divided into cholinergics and dopamine agonists. Cholinergics work by the blocking or competing at central acetylcholine receptors; dopamine agonists work by dec...

ANTIPARKINSONIS M AGENTS Created by: Group 2  WHAT IS ANTIPARKINSON AGENTS? Antiparkinson agents are divided into cholinergics and dopamine agonists. Cholinergics work by the blocking or competing at central acetylcholine receptors; dopamine agonists work by decarboxylation to dopamine or by activation of dopamine receptors; monoamine oxidase type B inhibitors work by increase dopamine activity by inhibiting MAO type B activity.  ADVERSE USES CONTRAINDICATIONS REACTIONS Side effects and adverse Persons with reactions vary widely among Antiparkinson agents hypersensitivity, products. The most common are used alone or in narrow-angle side effects include combination for glaucoma, and involuntary movements, patients with undiagnosed skin headache, numbness, Parkinson's disease. lesions should not use insomnia, nightmares, these products. nausea, vomiting, dry mouth, and orthostatic hypotension.  PHARMACOKINETICS PRECAUTION S Onset, peak, and duration INTERACTIONS Antiparkinson agents vary widely among should be used with products. Most products caution in pregnancy, are metabolized in the lactation, children, renal, liver and excreted in urine. Please check individual cardiac, hepatic disease, monographs since and affective disorder. interactions vary widely among products.  NERIC NAME E G NERIC NAMES GE Amantadine S Benztropine mesylate Biperiden Biperiden lactate Bromocriptine mesylate Levodopa AMANTADINE ACTION USES ADVERSE EFFECTS Prophylaxis or treatment of CNS: headache, dizziness, drowsiness, Prevent uncoating fatigue, anxiety, psychosis, depression, influenza type a, of nucleic acid in hallucinations, tremors, convulsions. viral cell, extrapyramidal CV: orthostatic hypotension, CHF reactions, INTEG: photosensitivity, preventing dermatitis penetration of parkinsonism, EENT: blurred vision HEMA: virus to host; respiratory tract leukopenia causes release of GI: nausea, vomiting, constipation, infection. dry mouth dopamine from GU: frequency, retention neurons. DOSAGE AND ROUTE: Influenza type a Extrapyramidal Adult and child > 9-years-old PO reaction/parkinsonism 200 mg/ day in single dose or divided bid Adult PO 100mg bid up to 400 mg per day in EPS; give Child 1 to 9 years old po 4.4 to 8.8 mg/kg/day divided bid-tid, not for 1 week then 100 mg as to exceed 200 mg/day needed in parkinsonism CONTRAINDICATION S ADMINISTER Hypersensitivity, Before exposure to influenza; continue for lactation, child < 1- 10 days after contact. year-old, pregnancy At least 4 hr before he to prevent insomnia After meals for better absorption, to (C) decrease GI symptoms. In divided doses to prevent CNS disturbances: headache, dizziness, fatigue, drowsiness.  BENZTROPINE MESYLATEUSES ACTION CONTRAINDICATIONS Parkinson symptoms, Blockade of central Hypersensitivity, extra- pyramidal ace- tylcholine narrow-angle glaucoma, symptoms associated receptors with neuroleptic drugs myasthenia gravis, GI/GU obstruction, child yr, peptic ulcer, megacolon, prostate hypertrophy DOSAGE AND ROUTE: Drug-induced extrapyramidal symptoms Adult: IM/IV 1-4 mg 1-2x day; Parkinson give PO dose as soon as possible; symptoms PO 1-2 mg bid/tid, increase by 0.5 Adult: PO 0.5-1 mg mg q5-6 days qd, increased 0.5 mg q5-6 days titrated to patient response  ADVERSE EFFECTS MS: Muscular weakness, cramping INTEG: Rash, urticaria, dermatoses MISC: Increased temperature, flushing, decreased sweating, hyperthermia, heat stroke, numbness of fingers CNS: Confusion, anxiety, restlessness, irritability, delusions, hallucinations, headache, sedation, depression, incoherence, dizziness, memory loss EENT: Blurred vision, photophobia, dilated pupils, difficulty swa lowing, dry eyes, mydriasis, increased intraocular tension, angle- closure glaucoma CV: Palpitations, tachycardia, hypotension, bradycardia Gl: Dryness of mouth, constipation, nausea, vomiting, abdominal dis- tress, paralytic ileus, epigastric distress GU: Hesitancy, retention, dysuria  ADMINISTER With or after meals to prevent GI upset; may give with fluids other than water At hs to avoid daytime drowsiness in patient with parkinsonism Undiluted IV (1 mg = 1 ml) dose at a rate of ≤1 mg/> 1 min; keep in bed for at least 1 hr after dose BIPERIDEN, BIPERIDEN LACTATE CONTRAINDICATIONS ACTION USES Parkinson symptoms, extra- pyramidal Hypersensitivity, narrow-angle Centrally acting symptoms secondary to glaucoma, myasthenia gravis, GI/GU competitive neuroleptic drug obstruction, child yr, peptic ulcer, anticholinergic therapy megacolon, prostate hypertrophy DOSAGE AND ROUTE: Drug-induced extrapyramidal symptoms Adult: PO 2 mg 1-3 times a day; Parkinson symptoms IM/IV 2 mg q30min, if needed, not Adult: PO 2 mg tidqid max to exceed 8 mg/24 hr 16mg/24 hr Available forms include: Tabs 2 mg; inj IM/IV 5 mg/ml (lactate)  ADVERSE EFFECTS CNS: Confusion, anxiety, restless- ness, irritability, delusions, hallucinations, headache, sedation, depression, incoherence, dizziness, euphoria, tremors, memory loss EENT: Blurred vision, photophobia, dilated pupils, difficulty swallowing, mydriasis, increased intra-ocular tension, angle-closure glaucoma CV: Palpitations, tachycardia, postural hypotension, bradycardia Gl: Dryness of mouth, constipation, nausea, vomiting, abdominal distress, paralytic ileus GU: Hesitancy, retention, dysuria MS: Weakness, cramping INTEG: Rash, urticaria, dermatoses MISC. Increased temperature, flushing, decreased sweating, hyperthermia, heat  ADMINISTER Parenteral dose with patient recumbent to prevent postural hypotension, give undiluted 2 mg or less/> 1 min IV With or after meals to prevent GI upset; may give with fluids other than water At hs to avoid daytime drowsiness in patient with parkinsonism  BROMOCRIPTINE MESYLATE ACTION USES CONTRAINDICATIONS Inhibits prolactin release by activating postsynaptic Female infertility, dopamine receptors; Parkinson's disease, Hypersensitivity to ergot, severe activation of striatal prevention of post- partum ischemic disease, pregnancy (D), dopamine receptors could be reason for improvement in lactation, amenorrhea severe peripheral vascular disease Parkinson's disease caused by Precautions: Lactation, hepatic hyperprolactinemia, disease, renal disease, children, acromegaly pituitary tumors PO: Peak 1-3 hr, duration 4-8 hr. DOSAGE AND ROUTE: Hyperprolactinemic indications Adult: PO 1.25-2.5 mg with 3 meals; may increase by 2.5 mg q.3- 7 days, usual 5-7.5 mg Acromegaly Adult: PO 1.25-2.5 mg x 3 days hs, may Parkinson symptoms increase by 1.25-2.5mg q3-7 days, usual range Adult: PO 2.5 mg qd-tid with meal x 14 or 21 days 20-30 mg/ day, max 100 mg/day Postpartum Adult: PO 1.25 mg bid with meals, may lactation increase q2-4 wk by 2.5 mg/day, not to exceed 100 mg qd  ADVERSE EFFECTS EENT: Blurred vision, diplopia, burning eyes, nasal congestion CNS: Headache, depression, restlessness, anxiety, nervousness, confusion, convulsions, hallucinations, dizziness, fatigue, drowsiness, abnormal involuntary movements, psychosisnence, diuresis GU: Frequency, retention GI: Nausea, vomiting, anorexia, cramps, constipation, diarrhea, dry mouth, GI hemorrhage INTEG: Rash on face, arms, alopecia CV: Orthostatic hypotension, decreased B/P, palpitation, extra systole, shock, dysrhythmias, bradycardia ADMINISTER With meal to prevent Gl symptoms At hs so dizziness, orthostatic hy potension do not occur PROCYCLIDINE HCI CONTRAINDICATIONS ACTION USES Hypersensitivity, narrow- angle glaucoma, my- asthenia Centrally acting gravis, GI/GU obstruction, child < 3 yr, megacolon, antichopyramidal Parkinson symptoms, disorders stenosing peptic ulcer, extrapyramidal prostatichypertrophy DOSAGE AND ROUTE: Adult: PO 2.5 mg tid pc, titrated to Available forms patient response include: Tabs 5mg  MS: Weakness, cramping ADVERSE EFFECTS INTEG: Rash, urticaria, dermatoses MISC: Increased temperature, flushing, decreased sweating, hyper- thermia, heat stroke, numbness of fingers CNS: Confusion, anxiety, restlessness, irritability, delusions, hallucinations, headache, sedation, depression, incoherence, dizziness, light-headedness, memory loss EENT: Blurred vision, photophobia, dilated pupils, difficulty swallowing, mydriasis, increased intra- ocular tension, angle-closure glaucoma CV: Palpitations, tachycardia, postural hypotension, bradycardia GI: Dryness of mouth, constipation, nausea, vomiting, abdominal dis- tress, paralytic ileus, epigastric distress GU: Hesitancy, retention, dysuria ADMINISTER With or after meals for GI upset; may give with fluids other than water At hs to avoid daytime drowsi- ness in patient with parkinsonism CARBIDOPA-LEVODOPA ACTION USES CONTRAINDICATIONS Decarboxylation of levodopa to periphery is inhibited by Parkinsonism resulting Hypersensitivity, narrow- carbidopa; more levodopa is from carbon monoxide, angle glaucoma, made available for transport chronic manganese to brain and conversion to undiagnosed skin lesions intoxication, cerebral dopamine in the brain arteriosclerosis DOSAGE AND ROUTE: Adult: PO 3-6 tabs of 25 mg carbidopa/250 mg levodopa qd in divided doses, not to exceed 8 tabs/ day Sus. Rel: 1 tablet BID at intervals of not less than 6 hrs usual: 2-8 tabs/day at Available forms include: Tabs intervals of 4-8 hr 10/ 100, 25/100, 25 mg carbidopa/ 250 mg levodopa Sus. Rel. tab: 50 mg/200 mg carbidopa/levodopa  ADVERSE EFFECTS HEMA: Hemolytic anemia, leukopenia, agranulocytosis CNS: Involuntary choreiform movements, hand tremors, fatigue, headache, anxiety, twitching, numbness, weakness, con- fusion, agitation, insomnia, nightmares, psychosis, hallucination, hypomania, severe depression, dizziness GI: Nausea, vomiting, anorexia, abdominal distress, dry mouth, flatulence, dysphagia, bitter taste, diarrhea, constipation INTEG: Rash, sweating, alopecia CV: Orthostatic hypotension, tachycardia, hypertension, palpitation EENT Blurred vision, diplopia, dilated pupils MISC: Urinary retention, incontinence, weight change, dark urine  ADMINISTER Drug up until NPO before surgery Adjust dosage depending on patient response With meals; limit protein taken t with drug Only after MAOIs have been dis continued for 2 wk; if previously on levodopa, discontinue for at least 8 hr before change to levodopacarbidopa LEVODOPA ACTION USES CONTRAINDICATIONS Decarboxylation to Parkinsonism, carbon dopamine, which monoxide, chronic Hypersensitivity, narrow- increases dopamine manganese intoxication, angle glaucoma, levels in brain cerebral arteriosclerosis undiagnosed skin lesions DOSAGE AND ROUTE: Adult: PO 0.5-1 g qd divided bidqid with meals, may increases by up to 0.75 g q3-7d not to exceed 8 g/day Available forms unless closely supervised include: Caps 100, 250, doses, not to exceed 8 tabs/ 500 mg: tabs 100, 250, day 500 mg  ADVERSE EFFECTS HEMA: Hemolytic anemia, leukopenia, agranulocytosis CNS:Involuntary choreiform movements, hand tremors, fatigue, headache, anxiety, twitching, numbness, weakness, confusion, agitation, inso0, nightmares, psychosis, hallucination, hypomania, severe depression, dizziness GI:Nausea, vomiting, anorexia, abdominal distress, dry mouth, flatulence, dysphogia, bitter taste, diarrhea, constipation INTEG: Rash, sweating, alopecia CV:Orthostatic hypotension, tachycardia, hypotension, palpitation EENT: Blurred vision, diploma, dilated pupils MISC: Urinary retention incontinence, weight change, dark urine  ADMINISTER Drug up until NPO before surgery Adjust dosage depending on patient response With meals; limit protein taken with drug Only after MAOIs have been discontinued for 2 wk ANTIEPILEPTIC AGENTS "Anti-convulsant" aka MECHANISM OF ACTION 1. Sodium channel blockers 3. GABA Inhibitors 4. GABA Analogues Sodium HYDANTOINS Channel Blockers AMINO SINE DERIVATIVES VALPROATE DERIVATIVES LAMOTRIGINE  Boxed Warning: Rapid IV administration 1. HYDANTOINS can result in hypotension and cardiac arrhythmias. Phenytoin Administered: Contraindications: - Orally or Intravenously Avoid use during pregnancy and in patients with: Sinus bradycardia Prodrug, Fosphenytoin Heart block Administered: Adams-Stokes syndrome - Intravenously or Intramuscularly.  Common Side Effects 1. HYDANTOINS Headaches ADDITIONAL SIDE EFFECTS: Dizziness Visual disturbances (e.g., blurred - Hepatotoxicity vision, nystagmus, diplopia) Gingival hyperplasia - Impaired metabolism of vitamin D, Client's Experience potentially causing osteomalacia hypersensitivity reactions, such as: Stevens-Johnson syndrome (SJS) Toxic epidermal necrolysis (TEN) - Reduced absorption of folic acid and Drug Reaction with Eosinophilia and vitamin B12, leading to hematologic Systemic Symptoms (DRESS) side effects (e.g., agranulocytosis, leukopenia, thrombocytopenia, and anemia)  2. AMINO SINE DERIVATIVES Carbamazepine - Orally or Intravenously. Important Side Contraindications: ▪︎ Pancreatitis Effects: Do not administer within 14 days ▪︎ Hepatotoxicity of monoamine oxidase inhibitors ▪︎Renal dysfunction (leading to fluid (MAOIs) or alongside non- retention and hyponatremia) nucleoside reverse transcriptase ▪︎Cardiovascular effects (e.g., inhibitors (NNRTIs) that are ⚠️ hypertension, AV block) CYP3A4 substrates, such as nefazodone. ▪︎ Avoid during pregnancy and use with caution in: ▪︎ Clients breastfeeding ▪︎ Those with alcoholism, cardiac, hepatic, or renal disease ▪︎ Children under 6 years of age  Common Side Effects: 3. Valproate Gastrointestinal issues (e.g., dyspepsia, nausea, vomiting, diarrhea, constipation) Hematologic issues (e.g., thrombocytopenia, leukopenia) Derivatives DRESS Valproic acid and Sodium Valproate Boxed warnings: Administered: Pancreatitis, - Orally and Intravenously. hepatotoxicity, and fetal toxicity (risk of neural tube defects. Contraindications: Avoid in pregnancy and in clients with: Urea cycle disorders Mitochondrial or hepatic  4. Lamotrigine - Orally. Common Side Effects: Boxed Warning: ▪︎ Headaches ▪︎ Dizziness Serious and life- ▪︎Dysmenorrhea threatening skin reactions Cause ▪︎Suicidal thoughts such as SJS and TEN ▪︎Hematologic side effects Precautions: Do not stop abruptly, as it may trigger uncontrolled seizures. Use with caution during pregnancy and in clients with: Severe depression Cardiac, hepatic, or renal disease CHANNEL BLOCKERS CALCIUM CHANNEL BLOCKERS 2. Orally or Intravenously. 1. SUCCINIMIDES LEVETIRACETAM SIDE EFFECTS: DRUG: Ethosuximide - Suicidal thoughts - Orally - SJS, TEN COMMON SIDE EFFECTS: - Hepatitis PRECAUTIONS: - Nausea, vomiting, diarrhea Avoid in clients who are - Headaches breastfeeding, and use with - Fatigue caution in pregnant women and those with cardiac, hepatic, or  DRUG: VIGABATRIN GABA - Orally. INHIBITORS - It inhibits GABA reuptake, increasing GABA concentration. SIDE EFFECTS: - Dizziness, weight gain, edema - Peripheral neuropathy - Life-threatening effects BOXED WARNING: - Risk of visual impairment GABA DRUG: GABAPENTIN ANALOGUES - Orally. SIDE EFFECTS: - Depression, amnesia, ataxia - Blurred vision, diplopia - Gastrointestinal issues Use with caution in pregnancy and client with renal disease  Do not stop medications abruptly, as it can trigger seizures. Patient Avoid alcohol and CNS depressants Counseling Monitor for mood changes and suicidal thoughts. Tips Teach about side effects such as gingival hyperplasia and bone loss, and emphasize oral hygiene. Advise clients on restricted foods like grapefruit juice for those on carbamazepine. Encourage regular vision checks for those on vigabatrin. MUSCLE RELAXANT WHAT IS MUSCLE RELAXANT? Musculoskeletal disorders may require surgical intervention for structural defects, but many conditions involving pain and spasms respond to skeletal muscle relaxants. Acute issues, like backaches, are treated with muscle relaxants, rest, physical therapy, and mild analgesics, typically for short-term use. These medications act on the central nervous system to reduce spasms and alter pain perception.  ADVERSE REACTIONS Drowsiness, dizziness, or dry Urinary problems, mouth, Weakness, Tremor, including enuresis, ataxia, seizures, Headache, frequency, or retention. Confusion, Nervousness, Hypersensitivity Slurred speech Blurred vision, Hypotension. reactions, including liver Gastrointestinal (GI) toxicity with dantrolene symptoms, including nausea, and tizanidine. vomiting, diarrhea, or Respiratory depression constipation PRECAUTIONS/CONTRAINDICAT INTERACTIONS IONS APPLY TO: Hypersensitivity to the muscle relaxant Pregnancy or lactation History of drug abuse Impaired kidney function Analgesics Psychotropic Liver disorders medications Antihistamines Blood dyscrasias Chronic obstructive pulmonary disease Cardiac disorders Older adults Abrupt discontinuation Closed-angle glaucoma GENERIC NAMES Balcofen Carisoprodol cyclone caprine dantrolene Methocarbamol BACLOFEN ACTION USES Inhibits synaptic CONTRAINDICATIONS responses in CNS by Spinal cord decreasing GABA, which injury, Hypersensitivity decreases neurotransmitter spasticity in function; decreases frequency, se- verity of multiple muscle spasms sclerosis DOSAGE AND ROUTE: Adult: PO 5 mg tid, then 10 mg tid, then 15 Available forms mg tid, then 20 mg tid , then titrated to re- include: Tabs 10, 20 sponse, not to exceed mg, 10 mg/20ml, 10 80 mg/day mg/5 ml  ADVERSE EFFECTS CNS: Dizziness, weakness, fatigue, drowsiness, headache, disorientation, insomnia, paresthesias, tremors EENT: Nasal congestion, blurred vision, mydriasis, tinnitus CV: Hypotension, chest pain, palpitations, edema GI: Nausea, constipation, vomiting, increased AST, alk phospha- tase, abdominal pain, dry mouth, anorexia GU: Urinary frequency INTEG: Rash, pruritus  ADMINISTER With meals for GI symptoms Gum, frequent sips of water for dry mouth CARISOPRODOL ACTION CONTRAINDICATIONS USES Depresses CNS by Hypersensitivity, blocking interneuronal Relieving pain, activity in descending stiffness in child 12 yr: PO 350 mg Available forms include: Tabs 350 mg  ADVERSE EFFECTS CNS: Dizziness, weakness, drowsiness, headache, tremor, depression, insomnia, ataxia, irritability EENT: Diplopia, temporary loss of vision CV: Postural hypotension, tachycardia GI: Nausea, vomiting, hiccups, epigastric discomfort INTEG: Rash, pruritus, fever, facial flushing  ADMINISTER With meals for GI symptoms  ACTION USES CONTRAINDICATIONS Unknown; may Acute recovery phase of Adjunct for relief myocardial infarction, be related to of muscle spasm dysrhythmias, heart antidepressant and pain in block, CHF, effects musculoskeletal hypersensitivity, child