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Pharmacology Unit5&6

Pharm Notes

Types of Opioid Receptors?(4) Mu:Analgesia(primary), Euphoria, Respiratory Depression, and Sedation. Kappa:Analgesia(primary) and Sedation. Delta: Analgesia(limited research. Sigma: Unwanted effects(dysphoria, hallucinations and confusion).
Opioids? alters the perception and emotional responses of pain due to receptors being in the CNS
Classification of Opioid drugs?(3) 1.Agonist(mimics/produce maximum effect). 2.Antagonist(block/reverse). 3.Agonist-Antagonist(mixing effects).
Agonist Opioids? Prototype?(2) Produce maximum effects of Mu and Kappa receptors. Prototypes:Morphine and Codeine.
Morphine's Indication?(5) Route(6) Pharmacokinetics?(3) Indication:severe pain, depress cough, pulmonary edema, MI(doesn't alter HR or BP) and antidiarrheal effects. Routes:PO, IM, IV SQ, epidural, and rectal. Kinetics:liver, kidneys, wide distribution.
Morphine common SE?(4) ADR?(4) SE:vertigo, faintness, light-headedness in ambulatory and puritus. ADR: Respiratory Depression, seizures, Tachycardia and confusion.
Other types of Agonist Opioids?(10) Codeine, Hydrocodone, Hydromorphone, Levorphanol, Oxycodone, Oxymorphone, Fentanyl, Methadone, Propoxyphene, Meperidine.
Codeine? (1) Hydrocodone? Hydromorphone?(1) Codeine: analgesic, antitussive, antidiarrheal effects, PO with milk. Hydrocodone: analgesic and antitussive. Hydromorphone: analgesic and antitussive. Faster onset of action and short duration.
Levorphanol?(2) Oxycodone?(1) Oxymorphone?(1), SE?(4) Administration?(1) Levorphanol: longer duration and smaller dose. Oxycodone: smaller doses than Codeine. Oxymorphone: antitussive. SE: N,V,less constipation, euphoria. Admin: PO with food or milk.
Fentanyl Types?(3) Warning?(1) Types:Sublimaze and Innovar (given with Anesthesia) and Duragesic(available as patch that last for 72hrs). Warning: when given IV too fast and in large doses can cause muscle rigidity of chest wall.
Methadone?(3) Propoxyphene?(3) Methadone: extended half-life, detoxification approved, give PO liquid. Propoxyphene:for mild-moderate pain, give with caution to those with excessive alcohol use, suicidal thoughts or prone to addiction.
Meperidine? Route?(1) Administration?(1) Adverse Reaction?(1)Contraindicated?(3) Monitor?(3) Helpful in those with acute asthma and GI/Biliary complications. Route: IM(rotate sites). Admin:large frequent doses. ADR: can lead to neurotoxicity. Contrain:liver dysfunction, COPD, chronic pain. Monitor:tachycardia, hypotension, behavior change.
Agonist-Antagonists?(3) Types(5?) Pharmacokinetics?(3) less potent analgesic, lower dependency potential and no severe withdrawal symptoms. Types:Butorphanol Tartrate, Dexocine, Pentazocine, Nalbuphine, Buprenorphine. Kinetics: liver, excreted, wide distribution.
Dezocine? Nalbuphine? Dezocine: IM, IV, added to CNS depressants. Nalbuphine: used for preop and OB.
Butorphanol Tartrate? Avoid giving to those who are?(3) Can be used with those who have?(1) Routes?(3) for moderate to severe pain. Avoid: MI, Narcotic dependent, or head injuries. Helpful: Gallbladder disease. Routes: IM, IV, nasal spary
Pentazocine? Avoid giving to those with?(4) combine with PO Narcan to prevent high incidence of abuse. Avoid: terminally ill, anxious, fearful, MI
Buprenorphine? Helpful Respiratory Stimulant?(1) dissociates slowly form Mu Receptors to block the effects of opioid agonist. Doxapram, not Narcan, can reverse respiratory depression from Buprenorphine.
Opioid Antagonists? Treatments?(5) Receptors?(3) SE?(4) reverse effects of agonist. Treats: opioid overdose, constipation, reverse respiratory depression, CNS depression or disease progression. Receptors: Mu, Kappa, and Delta. mainly Mu. SE:Hypertension, Tachycardia, HA and Hallucinations
Opioid Types?(3) Nalmefene, Naloxone, Naltrexone
Nalmefene?(2) Naloxone?(4) Naltrexone?(2) Nalmefene: IV onset 2-5mins, IM/SQ onset 5-15mins. Naloxone: Inactivated by PO, given Parenterally. IV onset 21-2mins, IM/SQ onset 2-5mins. Naltrexone: indicated for detoxifiedand opioid dependent clients, only one given PO.
Opioids Withdrawal Symptoms?(10) chills, hot flashes, Piloerection(goose bumps), Rhinorrhea, Mydrasis, lacrimation, anxiety, sweating, craving for drug, muscular twitching.
Nonopioid centrally acting analgesics? relieve moderate to severe pain without using opioid receptors.
Nonopioid types(1)? Route?(1) SE?(5) Type:Tramadol. Route: PO. SE:sedation, dry mouth, constipation, HA, minimal Respiratory Depression.
Nonopioid Contraindicated? Contra: seizures, MAOI, Intoxication to alcohol, sedatives, opioids, psychotropic drugs, sensitivity to opioids, hx of substance dependency.
Cyclooxygenase?(1) Cyclooxygenase Inhibitors Types?(1) Effects?(3) Mechanism?(1) ADR?(3) Enzyme: that produces prostaglandins(promote inflammation and pain). Type:aspirin. Effects: suppress inflammation, relieve pain, and reduce fever. Mech: Inhibition of Cyclooxygenase ADR: Gastric Ulceration, Bleeding, Acute Renal Failure.
Cyclooxygenase forms?(2) Cox-1:(good) found in all tissues and helps to regulate processes. Cox-2:(bad) found in tissues that are injured to produce inflammation and perception of pain. Also present in the brain to mediate fever and perception of pain.
Results from inhibiting Cox-1? Cox-2? Cox-1: gastric erosion/ulceration, bleeding tendencies, acute renal failure, and lack of protection against MI. Cox-2:suppression of inflammation, alleviate pain and reduce fever.
Cyclooxygenase Inhibitors categories?(2) 1.reduce inflammation:(NSAIDS)Aspirin, Ibuprofen, Naproxen and Celecoxib. 2.cannot reduce inflammation: Acetaminophen.
First Generation NSAID? Prototype?(1) Use?(3) Pharmacokinetics?(3) NSAID: inhibit both Cox-1/2. Prototype: Aspirin. Purpose: suppress inflammation(larger doses), relieve pain, reduce fever, dysmenorrhea, colorectal cancer, antiplatelt. Kinetics: sm.intestine, protein bound(allowing other durgs to work better),kidneys.
Aspirin ADR GI?(3) Bleeding?(1) Renal?(4) Salicylism?(4) GI:most common, gastric distress, heartburn, and nausea. Bleeding:supressing platelet aggregation. Renal:inhibits kidney function, blood flow, filtration and ischemia. Salicylism:tinnitus,sweating, HA, resp alkalosis.
Aspirin ADR: Reye's Syndrome?(1) Pregnancy?(1) Hypersensitivitiy?(4) Reye:do not give to children suspected of having influenza or chickenpox. Pregnancy: D-benefits out weight the harm. Hyper:asthama, hay fever, chronic urticaria, nasal polyps.
Aspirin Contraindicaiton?(1) Interations?(2) Lethal Dose(2) Routes?(2) Contra:bleeding disorders, allergy to ASA. Interaction: intensifies with warfarin. Dose:20-25gm adults, 4gm children. Routes: PO(different types of tablets) and PR(suppository).
Nonaspirin NSAID? Prototype?(1) Differ from ASA?(3) Indication?(1) NSAIDS with fewer ADR. Type: Ibuprofen. Differ:expensive, less GI bleeding and tinnitus, cause less inhibition of platelet aggregation. Indication:inflammatory disorders.
Second-Generation NSAID? Type?(1) Pharmacokinetics? (2) Indicated?(2) Selectivity for COX-2, suppress inflammation and pain with minimal risk for ADR. Type: Celecoxib. Kinetics: liver and kidneys. Indicate: OA and RA only.
Celecoxib contraindication?(2) SE?(6) contra: 3rd trimester pregnancy, allergic to sulfa. SE:Dyspepsia(impaired digestion), abdominal pain, renal toxicity, edema, Warfarin, cardio effects.
Drugs w/o anti-inflammatory properties?(1) Action?(1) Indicated?(2) Pharmacokinetics?(4) ADR?(1) Type: Acetaminophen. Action: inhibits prostaglandin formation in the CNS. Indicat: mild pain and fever. Kinetic: easily absorbed, easily distributed, liver and kidneys. ADR: rare at therapeutic dose
Acetaminophen Overdose? Overdose amount? Early Symptoms?(6) Early Symptoms Time? Late Symptoms?(3) Late Symptoms Time? causes severe liver damage. Amt: 4gms/day Early:sweating, anorexia, N/V/D, discomfort E-Time: 6-14hrs after ingestion. Late: swelling, tender, pain in abd area. L-Time: 2-4 days after ingestion.
Acetaminophen Overdose Treatment Steps?(4) (1) admin 17 doses of Acetycysteine(mucomyst). (2) admin gastric lavage or emesis. (3) serum levels (>150ug/ml)=hepatotoxicity. (4) perform Liver, Renal and Cardiac function test.
Osteoarthritis? Risk?(6) How many HCP visits a year? Nonpharmacological Therapy?(4) OA: slowly progressive MS disorder that deteriorates the articular cartilage and underlying bone. Risk: age, female, obese, family hx, sports injury, previous joint damage. HCP: 4x year Nonpharm: education, joint supports, PT, diet/ lifestyle changes.
OA Pharmacological Therapy?(6) Capsaicin, Aspirin, Acetaminophen, Corticosteroids, Experimental, and alternatives
Capsaicin? Administration?(3) Contraindications?(1) ADR?(2). topical analgesic for RA/OA, prevents/depletes Substance P(pain impulses) production. Admin:3-4x day, wear gloves, avoid eyes/broken skin. Contra: allergy to hot peppers. ADR: cough, burning(increased with heat, warm water, humidity and clothing)
In OA, Aspirin? Acetaminophen? ASA: Initial choice for OA in large doses. Acetaminophen: has weak anti-inflammatory action so beneficial in OA.
Corticosteroids? Caution? Administration?(2) benefits in OA by helping with flare up with less toxicity. Caution: repeated use can increase the acceleration of the disease. Admin: Oral route is non beneficial in OA. Intraarticular injections helps with OA.
Experimental(1) and Alternative(3) Pharmacological use for OA? Experi: helps to modify the disease process. Alter: fish oil, nettle leaf, ginger, willow bark.
Hyaluronate Injections? Does it help with OA? Administration?(1) acts as a lubricant and shock absorber. OA: NO. Admin: injected into the knee to offer pain relief for several months.
Gout? Hyperuricemia cause?(2) Gout drugs either?(2) recurrent Inflammatory disease caused by hyperuricemia. Hyper: (1) excessive uric production, (2) impaired renal excretion. Drugs: either relieve inflammation or reduce uric acid.
Types of anti-inflammatory drugs for Gout?(2) The first Type? Use?(3) ADR?(4) The Second Type? SE?(2) Colchicine: only for gout, inhibits leukocyte infiltration. Use:1.treat attacks(within hrs), 2.reduce recurrent attacks(taken qd), 3.abort impending attacks(taken q2hrs). ADR? N/V/D, abd discomfort. Indomethacin:suppress inflammation. SE: HA, GI ulcer
Types of anti-Hyperuricemia drugs for Gout?(3) First Type?(1) Use?(3) ADR?(2) SE?(3) Administration?(1) Allopurinol/Probenecid/Sulfinpyrazone Allo: inhibits uric acid. Use:Tophaceous Gout, imbalanced blood, cancer therapy. ADR:hypersensitivity, may cause attacks in the 1st few mths. SE: GI, Neuro, and Cataracts. Admin: with 2,000ml fluid/day.
The last two type of anti-Hyperuricemia drugs for Gout?(2) Use?(1) SE?(3) Drug Interactions?(2) Probenecid/Sulfinpyrazone. Use: increase excretion of uric acid. SE: Mild N/V and anorexia, take with food. ADR: exacerbate/induce attacks, hypersensitivity, renal injury Interact: dont take with ASA, reduce indocin dosage if taken with probenecid.
AED/Anticonvulsants?(2) Goal for TX?(1) Picking type of drug?(1) Why monitor plasma blood levels?(4) Types?(2) AED: suppress neurons during a seizure, suppress propagation of seizure activity. Goal: reduce to live normal/near normal life. Drug: trial period Plasma levels: dosage levels, cause of lost control, pt adherence and toxicity. Type: traditional/new
Traditional AED? Types?(6) Trad: effective, intolerable SE, long list of drug interaction, less safe in pregnancy and cheap. Types:Phenytoin, Barbiturates, Valproic acid, Carbamazapines, Ethosuximide, Primidone, Benzodiazepines.
Newer AED? Types(8) New: effective, tolerable, SE, limited drug interaction, safer in pregnancy, and expensive. Types:Oxcarbazepine, Lamotrigine, Gabapentin, Pregabalin, Levetiracetam, Topiramate, Tiagabine, Zonisamide.
Phenytoin?(3) Routes?(4) Therapeutic Range? Drug Interaction?(3) Traditional AED, inhibits Na Routes:PO(with food), IM(not recommended), IV(not >50mg/ml), SubQ(never). Range:10-20mcg. Inter: BC, Warfarin, and ETOH.
Phenytonin Drug Interaction?(3) teaching(1) inter:decreases warfarin effects, increase OC in women, ETOH increase metabolism. Teach: cautious in liver disease,
Barbiturates? Therapeutic Range? SE?(1) Route?(2)Contraindications?(1) Traditional AED that is a downer,long last, GABA. Range:15-45mcg. SE:drowsiness. Route: PO, IV(no> 60mg/ml). Con:child/pregnancy
Valproic Acid? Treat?(3) Therapeutic Range? Contraindicated?(1) Taditional AED, blocks Na/Ca and increases GABA. Tx:ABSENCE. Range:40-100mcg. Contra: pregnancy.
Carbamazapines? Therapeutic Range? Assessments(1) Nursing Interventions?(2) Traditional AED, #1 for Partial, pain and hard to control seizures. Range:4-12mcg. Assess: Skin for S-J syndrome. NI: blood counts, hematologic toxicity.
Ethosuximide? Therapeutic Range? Administration?(1) SE?(5) Use?(1) Nursing Intervention?(1) Traditional AED. Range:40-100mcg. Admin:PO take with meals. SE: N/V, drowsy, anemia, discolored urine. Use: Perfect drug for ABSCENCE seizures in CHILDREN and adults. NI:CBC
Primidone? Therapeutic Range? Drug Interaction?(1) Traditional AED, nearly identical to Barbiturates, so never take them together. This is a adjunct drug with other AEDS. Range:5-15mcg. Inter:CNS depressants.
Benzodiazepines? Types?(3) Traditional AED that must be used as adjunct, not a sole drug. (1) Diazepam: acute tx only. (2)Clonazepam: used for long-term. (3)Lorazepam: for anxiety,assess Vs baseline.
Oxcarbazepine? Administration?(1) Drug Interaction?(3) Contraindicated?(3) New AED block Na channels. Administration: can be taken mono or with adjunct with other AEDS. Inter:OC and ETOH. Contra:pregnancy and breast feeding, using lasix drug.
Lamotrigine? Indication?(4) New AED, blocks Na and Ca channels to decrease glutamate. Indicate: in adjunction tx for partial, generalized, tonic/clonic seizures and bipolar disorders.
Gabapentin? Indication?(2) ADR?(3) Caution?(1) New AED with unknown action. Indicat: partial seizures.neurological pain ADR:Somnolence, nystagmus, peripheral edema. Caution: driving or hazardous activity.
Pregabalin? Indication?(3) Adverse Effects?(4) Caution?(1) Drug Interaction?(1) New AED.Inter: . Inidcate: adjunction for partial seizures, neuropathic pain and fibromyalgia. Adverse:somnolence, blurred vision, edema, reproduction effects. Caution: risk for physical dependence. Drug:CNS depressants.
Levetiracetam? Indication?(4) Drug Interaction?(1) New AED with unique unknown action. Indicate:seizures, migraines, bipolar disorder and Peds epilepsy. Drug:none! good for patients with polypharmacy.
Topiramate? Indication?(3) Caution?(1) Adverse Effects?(3) New AED, USES ALL 4 MECHINISIMS. Indicate:partial and tonic/clonic and migraines. Caution: may cause seizures in those who take as mono treatment. ADR:somnolence, wt loss and closed angel glaucoma.
Tiagabine? Indication?(1) Adverse Effects?(1) New AED that blocks the reuptake of GABA. Adjunct. Inidcate:partial. ADR: may cause seizures in people w/o seizures on mono treatment.
Zonisamide? Indication?(1) Adverse Effects?(2) Contraindicated?(3) New AED that blocks Na and Ca channels. Adjunct. Indicate:partial. ADR: depression, suicide. Contra: allergy to sulfonamide, pregnancy or breast feeding.
Overall Teaching(6) 1.take med as ordered. 2.Keep seizure chart. 3.avoid driving/hazardous activites. 4.never discontinue w/o permission. 5.carry extra med. ETOH or CNS depressants.
Created by: aneshia



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