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97 Cards in this Set
- Front
- Back
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Parkinson's Disease |
- progressive disorder of muscle movement d/t reduced dopamine - s/s - tremors, muscle rigidity, bradykinesia and postural and gait abnormalities - treat - temporary relief of symptoms, not cure - pharm - restore dopamine |
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Levodopa/Carbadopa |
- enhance synthesis of dopamine in surviving neurons - levodopa replaces dopamine, carbidopa diminishes metabolism in GI tract to negate SE s/e - hypotension, n/v, tachycardia, (visual & auditory), dyskinesia |
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Dopamine Receptor Agonists (ropinirole- Requip, pramipexole-Mirapex) |
- monitor renal function esp. if on ACE inhibitor - Caution with statins or other P450 drugs |
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Anticholinergic Agents (Cogentin) |
- Caution in elderly d/t urinary retention esp. BPH - Precipitates narrow Angle Glaucoma |
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General Points in Treatment of Parkinson's |
- Carbidopa/levodopa most effective (1st line) - Pramipexole/ropinirole: early and late - Amantadine: mild symptoms - Anticolinergics: limited use d/t ADE - COMT inhibitors: increased dyskinesias |
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Alzheimer's Disease |
- dementia: plaques, loss of neurons - treat: aimed at improving cholinergic transmission; preventing cytotoxic actions - palliative, no agents alter process of disease, modest short term benefit |
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Acetylcholinesterase inhibitors donepezil - Aricept, rivastigmine, and galantamine |
- mild to mod AD - block enzyme that degrades acetylcholine (enhances cholinergic transmission) - improves function and slows progression for a while - ADE: GI (N/V), diarrhea, insomnia, fatigue - precautions: history of ulcers, Asthma, conduction problems |
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NMDA receptor antagonist Memantine - Namenda |
- moderate to severe AD, can be given in addition to acetylcholinesterase inhibitors - block cytotoxic effect; prevents loss of neurons - ADE: does not inhibit CYP450, 100% bioavailable w/ or without food; constipation confusion, dizziness, HA - dose reduction with severe renal impairment |
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Treatment principles in Alzheimer's Disease |
- Acetylcholinesterase inhibitors stabilize for about a yr then add memantine - treat concurrent depression, delirium - avoid sedating or anticholinergic meds - avoid abrupt d/c of these meds (worse quick) - drug interactions CYP450 |
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Epilepsy Goals & Drug classes |
- eliminate seizures and provide optimal QoL; balance drug and ADE - Hydantion - phenytoin, Succinimide - ethosuximide, GABA analogs, carbamazepine - Tegretol, Keppra, Barbituates - phenobarbital, benzodiazipines - diazepam (Valium) |
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Mechanism of Action of Antiepileptic Drugs |
- increase the threshold of the CNS to convulsive stimuli or inhibit the spread of seizure activity - block Na+ Ca+ voltage gated channels - enhance inhibitory impulses - interfere with excitatory glutamate transmission - multiple targets - suppress seizure activity, Do NOT cure
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Factor involved with choice of therapy in Epilepsy |
- class of seizures - patient variables (age, comorbidities, cost) - treat seizures differently - several drugs may be equally effective so based on toxicity, cost comorbidity, drug interactions |
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Treatment Principles in Epilepsy |
- monotherapy better adherence - appropriate to type - least toxic - titrate dose upward - not needed if only 1 seizure, after 2 start - d/c seizure free 2-5yr, normal neuro exam - withdrawal gradually to prevent seizures |
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Phenobarbitol |
- used in prevention of febrile seizures in children (given according to how quickly temp rises not necessarily how high temp is) quick elevation in temp can result in seizures - not routine, just used during acute febrile |
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Phenytoin |
- zero-order pharmacokinetics: small increase in daily dose - can produce large increase in plasma concentration, resulting in toxicity - monitor: Vit D, folic acid, thyroid - considerations: shake a suspension, can cause hirsuitism and impaired congnition and gingival hyperplasia - pregnancy and lactation concerns: causes Vitamin D deficiency, folic acid deficiency |
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Migraine Headaches |
- w/ or w/o aura (visual, sensory, and/or cause speech or motor disturbances) - severe, unilateral, pulsating HA lasts 2 hours to days accompanied with N/V, photophobia, phonophobia - spreading depression of neuronal activity accompanied by reduced blood flow (hypoperfusion) that leads to hyperperfusion (arterial dilation) |
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Abortive agents for Migraine HA (Triptans - sumatriptan) |
- HA already started, trying to stop; serotonin receptor agonists, result in vessel constriction - Contraindication: heart disease or anything bothered by vasoconstriction, pregnancy, uncontrolled HTN - Warnings: do Not give if CVD risk factors unless r/o CAD, consider 1st dose in office and ECG after administer caution in renal or hepatic impairment - ADE: chest pain, vasospasm, MI, VT, Vfib, TIA, seizure, hypertensive emergency, dizziness, fatigue, flushin, HA, nausea, dry mouth, somnolence
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Migraine Treatment |
- simple HA respond to NSAIDs - ASA, ibuprofen, naproxen, diclofenac - combo acetaminophen/aspirin/caffeine most consistent efficacy - Acetaminophen alone not recommended |
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Ergots (Caergot) |
- mod to severe; alpha adrenergic blocking effect of smooth muscle peripheral and cranial vessels; vasoconstriction - contraindications: do not use w/in 24hrs of triptan; same as triptan - warnings: vasospasm, overuse results in ergotism (intense arterial constriction - peripheral ischemia, pain, pallor - can progress to gangrene) - precautions: can result in dependence and abuse |
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Migraine Prophylaxis |
- recurring migraines produce significant disability, using 2x/wk or more, getting a lot of SE, if predictable pattern - (1st) B-blockers, Ca Channel Blockers, tricyclic antidepressants (2nd) SSRI antidepressants, anticonvulsants |
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Treatment Principles of Migraine |
- mild to mod: NSAIDs, ASA or combo - n/v use nasal spray or injection or add antiemetics - Triptans are first line: fewer ADE - Take at earliest onset of HA - Abortive agent should not be given more than 2x/wk |
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How Migraine Prophylaxis Agents work |
B-Blockers - stabilize vascular tone Ca Channel Blockers - regulate vascular smooth muscle contraction, neurotransmission, and hormone enzyme activity Tricyclic Antidepressants - increase availability of synaptic NE or serotonin; down regulation Selective serotonin Receptor Inhibitors - prevent venoconstrictive effect of decreased serotonin levels Anticonvulsants - exert activity through their influence on cerebral arteries and circadian rhythyms; may help regulate secretion of hormones |
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Antidepressant SSRI fluoxetine HCL (Prozac), citalopram (Celexa), escitalopram (Lexapro), paroxetine (Paxil), sertraline (Zoloft) |
- block reuptake of serotonin; take at least 4wks to work up to 12wks - half-life of fluoxetine vs others: much longer, up to 50 hrs and metabolite up to 10 days; once weekly dosing (good for compliance) - ADE: HA, sweating, anxiety, agitation, GI (N/V/D), weakness, fatigue, sexual dysfunction, sleep disturbancs (insomnia and somnolence) - caution/warning: children and teens more suicidal; do not give with MAOI - discontinuation syndrome: if abrupt withdrawal |
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Atidepressant SNRI venlafaxine SR (Effexor SR), duloxetine (Cymbalta) |
- inhibit serotonin and norepinephrine; use if SSRI not effective - ADE: nausea, HA, sexual dysfunction, dizziness, insomnia, sedation, and constipation, dry mouth, somnolence, diaphoresis, possible risk in increase in blood pressure or heart rate |
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Atypical Antidepressants Bupropion (Wellbutrin) Mirtazapine (Remeron) Trazadone |
- weak dopamine and NE inhibitor - ADE: dry mouth, sweating, nervousness, tremor, low incidence of sexual dysfunction, increased risk for seizures at high doses - enhances serotonin and NE; sedating - ADE: increased appetite and weight gain - weak serotonin inhibitors; mildly sedating - ADE: priapism
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Tricyclic Antidepressants (TCAs) nortriptyline (Parnate) |
- block NE and serotonin, a-adrenergic, histaminic - other uses: panic disorder, chronic pain, bedwetting in kids, migraine, diabetic neuropathy
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Depression Treatment in Specific Populations |
Geriatrics: watch for confusion, drug interaction, increased risk of toxicity Pediatrics: don't use tricyclic until <12y.o.; SSRI >18yrs, fluoxetine >8yrs. Black Box warning: increased suicide risk Pregnancy and lactation: cat C & D |
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Benzodiazepines |
- use: reduce anxiety, sedative and hypnotic, anterograde amnesia (procedures), anticonvulsant, muscle relaxant (Baclofen & Diazepam), phobia, ETOH withdrawal - ADE: drowsiness, confusion, ataxia, cognitive impairment - precautions: do not abruptly discontinue, liver disease, acute narrow angle glaucoma, alcohol and other CNS depressants |
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buspirone (Buspar) |
- use: generalized anxiety disorder (takes up to a week to work) - ADE: low - HA, dizziness, nervousness, light-headedness |
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zolpidem (Ambien) |
- GABA-BZ Receptor Agonist - few withdrawal effects, min rebound insomnia, little or no tolerance w/prolonged use - caution in renal impairment - rapidly absorbed GI and short half-life, hepatic metabolism CYP450 system - ADE: nightmares, agitation, HA, GI upset, dizziness, daytime drowsiness |
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zaleplon (Sonata) |
- really short half-life, about an hour - few effects |
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Typical (Phenothiazines, Thioxanthenes, Phenylbutylpiperadines) vs Atypical (Dibenzepines, Benzisoxazoles, Quinolinones) Neuroleptic drugs |
Typical are old ones, convention, first generation, MOA unknown, affect variety of receptors Atypical are newer ones, second generation, fewer ADE, work on serotonin and dopamine |
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Treatment Recommendations for psychosis |
- typical and atypical equally effective - Atypicals generally preferred 1st line - one doesn't work, try another - therapeutic effect measured by patient functional abilities and decreased symptoms - generally takes 3 week to work - initially responsive pts may relapse - dose increase until therapeutic then decrease for long term |
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Nonsteroidal Anti-Inflammatory Drugs
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- Difference between ASA and others: reduces pain centrally, blocks IL-1 for temp control, anti-platelet (irreversible inactivation of Cox-1 for life of platelet) - Cox 1 Inhibition: - Cox 2 Inhibition: inhibit prostaglandin synthesis - decrease sensitivity of blood vessels to bradykinin and histamine, affect T lymphocytes & reverse vasodilation of inflammation - mild to mod pain, soft tissue injury, dental pain, minor surgery, OA, RA, dysmenorrhea, gout |
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Osteoarthritis |
- degeneration of articular cartilage, body attempts to repair; hypertrophy, thickening, inflammation occurs - first line treatment: acetaminophen NSAIDS COX-2 Inhibitors Intraarticular injection of steroids |
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Gout |
- inflammatory response to precipitation of urate crystals in tissues - acute management: NSAIDs, colchicine, glucocorticosteroids - treat hyperuricemia after acute attack - Preventive: colchicine, uricosuric drug or allopurinol |
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Colchicine |
- decreases deposition of uric acid and reduces inflammatory response (no effect on uric acid metabolism and not an analgesic) - ADE: diarrhea, n/v, abdominal pain - Drug interactions: enhances CNS depressants and sympathomimetic agents; may interfere w/VitB12 absorption, increase cyclosporine - toxicity increased w/ clarithromycin, erythromycin, and grapefruit juice |
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Xanthine Oxidase Inhibitor allopurinol & febuxostat |
- for acute gout; reduces production of uric acid (give with colchicine) - contraindications: prior severe rxn - warnings: hepatic and renal history - ADE: bone marrow suppression, nausea, rash - monitoring: renal function w/ thiazide diuretics |
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Uricosuric drugs Probenecid |
- inhibit the secretion of weak acids and reabsorption of uric acid, increases urinary excretion (chronic gout); give with colchicine - contraindications: blood dyscrasias, hx of uric acid stones, on high dose ASA therapy - warnings: may exacerbate or prolong acute gout (use of Colchicine reduces risk); do Not use salicylates, caution with PUD - monitoring: Uric Acid levels every 2-3mo, renal and hepatic function |
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Osteoporosis Risk Factors |
- postmenopausal Caucasian women - personal history of fracture as an adult - history of fragile fracture in 1st degree relative - low body weight (<127 lbs) - current smoking - use of oral corticosteroid therapy for >3mos. - estrogen deficiency at early age (<45 yrs.) - dementia - poor health/fraility - recent falls - low calcium intake - low physical activity (para/quadriplegic) - alcohol >2 drinks/day - anorexia |
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Bisphosphonates alendronate sodium (Fosamax) risedronate (Actonel) ibandronate sodium (Boniva) zoledronic acid (Reclast) |
- decrease osteoclastic bone resorption; small but significant gain in bone mass (preferred for postmenopausal) - taken on an empty stomach, sit up 30min - ADE: severe bone, joint, muscle pain; osteonecrosis of jaw w/delayed healing - Contraindications: hypocalcemia, renal insufficiency, unable to stand or sit for 30 - 60 min., esophageal abnormalities, malnutrition |
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Calcitonin (Miacalcin, Calcimar, Osteocalcin) |
- reduces bone resorption (less effective) - Unique Property: relief of pain w/ osteoporotic fracture |
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Selective Estrogen-Receptor Modulators (SERMs) raloxifene (Evista) |
- increases bone density; reduces LDL cholesterol concentration - ADE: hot flashes, leg cramps, increased chance of venous thromboembolic events - Contraindications: DVT, PE, allergy to calcitonin |
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Parathyroid Hormone teiparatide (Forteo) |
- bone formation; increases spinal bone density and decreases vertebral fracture risk - indication: osteoporosis & steroid induced - precautions: increased risk of osteosarcoma, Pagets disease, hx of bone cancer, hypercalcemia - ADE: nausea, dizziness, cramps, injection site pain |
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Muscle Relaxants: Patient Variables |
geriatrics: - caution more susceptible to sedative effects of muscle relaxers, increased risk of falls pediatrics: - safety not established in children <12 yrs. old pregnancy and lactation: - safety not established
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Antispasmotics CNS depressants: metaxalone (Skelaxin) methocarbamol (Robaxin) TCA relative: cyclobenzaprine (Flexeril) |
- indication: musculoskeletal conditions as adjunct to rest, comfort measures; musculoskeletal pain, muscle spasm - effect through production of sedation |
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Antispasmotics and Antispasticity Benzodiazepine: diazepam (Valium) a2-Adrenergic agonist: tizanidine (Zanaflex) |
- muscle spasm; spasticity - works directly on skeletal muscle - diazepam is only benzo used for direct skeletal muscle relaxant and spasticity by upper motor neuron disorders |
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Antispasticity GABA receptor stimulant: baclofen (Lioresal) |
- spasticity resulting from MS and spinal cord trauma (CNS disease) |
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Major classes of immunosuppressive drugs used in transplant |
glucocorticoids calcineurin inhibitors: suppresses T cells anti-proliferative/antimetabolic agents: inhibits T cells, effect last several months after stopped biologicals (antibodies) |
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Pathophysiology of autoimmunity, autoimmune diseases |
- when body mounts an immune response against itself due to failure to distinguish self tissues and cells from foreign (non-self) antigens - RA, Myasthenia Gravis, Psoriasis, Lupus (SLE), type I DM, MS |
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Methotrexate |
- Folic acid antagonist: anti-inflammatory and immunosuppressive properties - do not use if childbearing age and trying (teratogenic) - contraindicated with renal disease - ADE: hair loss, nausea, oral ulcers, bone marrow suppression, hepatotoxicity, lung disease |
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Prednisone |
- take with food to avoid GI upset - take consistently and in morning (for circadian rhythm) |
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Disease Modifying Anti-rheumatic Drugs |
DMARDs, Corticosteroids, and Immunomodulators |
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Patient Education for Immunosupression |
- Purpose - Lifelong therapy - Infection prevention and malignancy - Cardiovascular risk reduction - Limiting sun exposure |
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Blood Brain Barrier Factors that influence drug penetration |
- Lipid solubility of drug (high lipophilicity = more) - Molecular weight of the drug (small = more) - Protein binding of the drug (Less = more) - Inflammation of the BBB (=leaky) |
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Bacteriostatic |
- Arrest the growth and replication of bacteria |
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Bactericidal |
- Kills the bacteria - Ex. B-lactams |
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Minimum Inhibitory Concentration |
- Lowest concentration of antibiotic that inhibits bacterial growth |
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Minimum Bactericidal Concentrations |
- lowest concentration at which an antimicrobial agent will kill a particular microorganism |
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Concentration Dependent Killing |
- increase in rate of bacterial killing as the concentration of the antibiotic increases - Aminoglycosides, Fluoroquinolones |
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Time Dependent Killing |
- Percentage of time that blood concentrations of the drug remain above the MIC; increasing concentration does not increase rate of kill - B-lactams, Glycopeptides, Macrolides, Clindamycin |
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Post Antibiotic Effect |
- persistent suppression of microbial growth that occurs after levels of antibiotic have fallen below the Minimum Inhibitory Concentration |
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Chemotherapeutic Spectra |
? |
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Combination Therapy |
- Use more than one drug for only one bug - Increases risk for infection - to ensure appropriately covered whatever resistant pathogen is growing - used when history of resistant pathogen |
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Synergy |
- each drug is good alone but together better than either one could be by their self - addition of gram negative to gram positive antibiotic to treat gram positive organism - ex endocarditis, low dose aminoglycoside added to vancomycin |
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Spectrum of Activity |
- Narrow: act only on a single or limited group; treatment of documented pathogen - Extended: effective against gram-positive organisms and a number of gram-negative - Broad: effect a wide variety of microorganisms (caution superinfection); EMPIRIC; use before organism known |
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Resistance |
- genetic alteration of the bacteria's own DNA sequence - proteins make diff binding sites - efflux pumps (bacteria find antibiotic and kick out) - enzymatic inactivations |
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Superinfections |
- caused by use of broad-spectrum agents and/or combination of agents - lead to alterations of the normal microbial flora - permits overgrowth of opportunistic organisms - Ex. yeast infections & C. Diff |
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Mechanisms of Resistance that bacteria exhibit |
- B-lactams: production of B-lactamase enzymes - Macrolide: active efflux, alter target sites - Tetracyclines: active efflux, ribosomal protective proteins, enzymatic inactivation - Aminoglycoside: alter uptake, modifying enzymes, alter binding sites - Clindamycin: altered target sites, active efflux - Linezolid: alter binding sites |
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Antimicrobial classes sites of action |
- B-lactams & Vancomycin: cell wall synthesis - Tetracyclines, Aminoglycosides, Macrolides: protein synthesis - Fluoroquinolones: nucleic acid synthesis (DNA) - Sulfonamides & Trimethoprimapole: metabolism |
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Factors determining selection of antibiotic agents |
- ID of the organism - Organism susceptibility - Site of infection - Patient Factors - Drug Safety - Cost of therapy - Empiric therapy v. treatment of infection - Route of Administration |
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Patient Factors influencing selection of agent |
- Immune system - Renal function - Hepatic function - Poor perfusion - Age - Pregnancy - Lactation |
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B-lactams PCN Cephalosporin Monobactams Carbapenems |
- bind to gram positive and negative cell wall - hypersensitivity (rash) to anaphylaxis to death - B-lactamase enzymes |
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Cephalosporins |
- Generation based on antimicrobial activity - 1st generation: effect gram positive - each subsequent covers more gram negative - 4th & 5th: cover gram negative and not positive - resistance to beta lactamase |
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Vancomycin |
- inhibit cell wall synthesis - bactericidal - covers gram positive only - ototoxicity - red man syndrome (red face and torso) r/t rate; symptoms resolve with dc or slowed rate |
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Tetracyclines Doxycycline Minocycline Tetracycline |
- bacteriostatic - avoid acid suppressants and dairy products - requires renal dosage - cross resistance - contraindicated in pregnancy, lactation b/c effects on calcified tissue (bone and teeth deposition in growing children)
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Aminoglycosides Gentamicin Tobramycin Amikacin Streptomycin |
- inhibits protein synthesis - bactericidal - post antibiotic effect - nephrotoxicity, ototoxicity |
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Macrolides Erythromycin Clarithromycin Azithromycin |
- inhibit protein synthesis - bacteriostatic - QTc prolongation |
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Clindamycin |
- inhibit protein synthesis - bacteriostatic - most associated with C-Dif |
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Oxazolidinones (linezolid - Zyvox) |
- covers gram positive organisms only - bacteriostatic - ADE: thrombocytopenia with tx >2wks - caution with SSRIs: serotonin syndrome |
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Glycyclines - Tigecycline (Tygacil) |
- bacteriostatic - covers everything but pseudomonas - tooth discoloration - increased risk of death |
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Fluoroquinolones Ciprofloxacin Levofloxacin Moxifloxacin |
- inhibit DNA synthesis - bactericidal - post antibiotic effects - not recommended in pediatrics d/t tendon rupture - older better than newer - covers atypical pathogens |
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TMP-SMX combination Bactrim |
- inhibit DNA synthesis - bacteriocidal - Steven's Johnson Syndrome (severe dermatologic reaction d/t sulfa allergy) |
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Metrondiazole |
- inhibits DNA synthesis - bactericidal - covers anaerobes - Disulfiram reaction with ETOH |
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Yeast |
- candida most common |
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Endemic Mycoses |
Histoplasmosis Coccidomycosis Blastomycosis |
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Opportunistic Mycoses
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Cryptococcosis Candidiasis Aspergillosis Zygomycosis |
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Polyenes Amphotericin B Lipid-based Amphotercin B Nystatin |
- targets cell membrane - does not penetrate CSF - premedicate with hydrocortisone or APAP - Neprotoxicity - admin fluids; less w/lipid based
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Pyrimidines Flucytosine |
- disrupts DNA synthesis - Fungistatic - combo w/Amphotericin - penetrates CSF - neurotpenia, thrombocytopenia, bone marrow depression, hepatic dysfunction |
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Azoles Itraconazole Fluconazole Voriconazole Posaconazole |
- targets cell membrane - fungistatic - AE: Voriconazole - visual disturbances, nephrotoxicity |
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Echinocandins Caspofungin Micafungin Anidulafungin |
- inhibit cell wall synthesis - IV only |
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Antivirals |
- viruses obligate intracellular parasites - invade host cells - generally more toxic - ALL virustatic - active only against replicating viruses |
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Acyclovir |
- renal toxicity w/IV - neurotoxicites |
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Amantadine & Rimantidine |
- blocks viral replication - use for Influenza A only - high levels of resistance |
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Oseltamivir & Zanamivir |
- Inhibits new viruses from infecting cells - Activity against Influenza A & B - should be administered/in 30 hours of symptom onset (not after 48 hours)
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Zanamivir (Relenza) |
- dry powder disk inhaler |
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Oseltamivir (Tamiflu) |
- oral tablet/suspension |
