Exam 3 Meds Flashcards

Question

Topical Agents Caused by S. aureus, S. pyogenes

Answer 1

Up to 5 lesions can be treated with mupirocin (Bactroban) More than five lesions would benefit from cephalexin

Answer 2

Can treat with topical nystatin or clotrimazole Topical options include miconazole and clotrimazole

Answer 3

Principle endogenous androgen responsible for promoting the growth and development of male sex organs and maintaining secondary sex characteristics

Answer 4

Indications • Male (primary) hypogonadism • Male (hypogonadotropic) hypogonadism • Delayed male puberty • Hormone therapy in transgender males (off-label use) • Endometriosis and some postmenopausal symptoms in women (not FDA approved) ``` Signs and symptoms • Low libido • Decreased morning erections • Low bone mineral density • Gynecomastia • Small testes • Loss of body hair • Fatigue, depression, anemia, reduced muscle mass, increased fat mass ``` ``` Low morning (8–10 a.m.) serum testosterone • Primary goal of testosterone therapy is to restore serum testosterone concentration to normal range • Testosterone therapy is indicated only for testosterone deficiency, not for impaired spermatogenesis ``` Virilization/sexualfunction Improvedmusclestrengthandreducedfatmass • Improves bone density • Effectisseenwithinthreetosixmonthsof therapy, except for bone density, which isn’t until 24 months ``` Adverse effects • Acne • Prostatedisorders • Sleep apnea • Erythrocytosis • Recommend against testosterone use on “trial” basis in healthy, middle-aged men ``` Can be given gel, IM, subcutaneous *not good to be given orally b/c its rapidly metablized Contraindications • Prostatecancer • Male breast cancer b/c prostate is responsive to testosterone- prostate will get even bigger and you have trouble peeing • Severelowerurinarytractsymptoms • Erythrocytosis (HCT over 50) • Severe,untreatedsleepapnea • Uncontrolled CHF Drug interactions • Anticoagulants • Diabetic agents • Corticosteroids *check levels 2-3 months after initiation, then 1/year...evaluate for prostate CA, check HCT

Answer 5

5-Alpha Reductase Inhibitors Treats BPH and male pattern baldness Inhibits enzymes that converts testosterone to DHT (dihydrotestosterone) Caution • Prostate evaluation required for any increase in PSA while on medication

Answer 6

GnRH Analogues Luteinizing hormone (LH)-releasing hormone antagonists • Creates reversible chemical orchiectomy state in males • Creates reversible chemical oophorectomy state in females Indications • Advanced prostate cancer • Advanced breast cancer • Management of endometriosis and uterine fibroids (leiomyomata) • Precocious puberty • Pubertal suppression in transgender adolescents

Answer 7

Aldosterone Antagonist, Part I Aldosterone antagonist and inhibitor of 5- alpha-reductase • Potassium sparing diuretic ``` Indications • Polycystic ovary syndrome • Acne • Hirsutism • Dosing • Orally 50–200 mg daily ``` Adverse effects • GI upset • Gynecomastia • Contraindicated in pregnancy (Category X)

Answer 8

Ethinyl estradiol: 20–35 mcg • Metabolized in liver • Monophasic, biphasic, triphasic • No significant difference in contraceptive efficacy • Start with lowest estrogen while maintaining cycle control • Dose may be increased if breakthrough bleeding occurs ``` Conditions that carry unacceptable health risk • Age over 35 and smoking • Uncontrolled HTN • Venous thromboembolism • Current breast cancer • History of stroke • Cirrhosis • Migraine with aura • Ischemic heart disease or multiple risk factors ``` Advantages: Highly effective contraceptive • Rapidly reversible • Regulate menstrual bleeding • Decreased menstrual blood loss and dysmenorrhea • Reduction in risk of ovarian and endometrial cancers

Answer 9

Metabolism is increased by any drug that increases liver microsomal enzyme activity • Commonly includes anticonvulsants • Efficacy of combined oral contraception (COC) is likely to be diminished if concurrently taking a drug with this effect • CDC recommends against women on anticonvulsants taking COCs for contraception • Rifampin is the only antibiotic proven to reduce serum EE and progestin levels • Griseofulvin, an antifungal, has been associated with contraceptive failure, but limited data

Answer 10

Indications • Vasomotor symptoms • Genitourinary symptoms • Benefits outweigh risk for healthy, symptomatic women who are within 10 years of menopause or younger than 60 years old and do not have contraindications to treatment • Long-term use for prevention of disease is no longer recommended ``` Formulations • Oral • Transdermal • Topical gels, emulsions, lotions • Intravaginal creams, tablets, rings • Consider type of estrogen and route of administration, as well as need for progestin ``` Systemic • Vasomotor symptoms • Oral or transdermal • Oral has greater effect on liver due to first-pass effect • Oral increases liver production of clotting factors, HDL, triglycerides, and proteins such as sex hormone-binding globulin (SHBG) and thyroxine-binding globulin (TBG) Systemic • Transdermal is associated with lower risk of venous thrombosis and stroke • Transdermal has less effect on serum lipids compared to comparable oral dose • Transdermal is equally effective to oral for preserving bone density Conjugated equine estrogens (CEEs): derived from pregnant mare’s urine, mostly comprised of estrone • Synthetic conjugated estrogens: derived from plant source (soy, yams) • Micronized 17-beta estradiol: structurally identical (bioidentical) to main product of premenopausal ovary • Esterified estrogens: comparable serum estradiol/estrone levels to conjugated estrogen • Ethinyl estradiol: more potent than others for MHT; therefore used in very low doses ``` Adverse effects • Breast soreness • Headaches • Elevated blood pressure • Exacerbation of diabetes • Cholestasis • Thromboembolic event • Endometrial hyperplasia ``` Contraindications History of breast cancer • Coronary heart disease • Venous thromboembolic event • Stroke/TIA • Active liver disease • Unexplained vaginal bleeding • High risk endometrial cancer

Answer 11

Selective estrogen receptor modulator (SERM) * Estrogen antagonist in breast: reduces risk of breast cancer * Increase in thromboembolism and hot flashes * No effect on heart disease or endometrium

Answer 12

Selective estrogen receptor modulator (SERM) Increases thickness and moisture of vaginal mucosa • Indication • Dyspareunia in postmenopausal females • Vaginal dryness in postmenopausal females • Oral 60 mg once daily • Estrogen agonist effect in endometrium • Potential increased risk of endometrial cancer if intact uterus • Increased risk of stroke and DVT

Answer 13

Thickens endometrium • Stabilizes endometrium • Thickens cervical mucous • Relaxes smooth muscle of uterus • Thins vaginal mucosa

Answer 14

Mechanism of action • Thickening cervical mucus to inhibit sperm migration • Suppress ovulation • Lower mid-cycle peak of FSH and LH • Slow egg movement through Fallopian tube • Thin endometrium Overall complication rates are low for all progestin-only methods Implant, IUD, depo-shot ``` Adverse effects • Irregular breakthrough bleeding • Breast tenderness • Galactorrhea • Nausea • Contraindications • Known or suspected pregnancy • Known or suspected breast cancer • Undiagnosed abnormal uterine bleeding • Benign or malignant liver tumors, cirrhosis, acute liver disease ``` Gabapentin,Levetiracetam,Valproate, Zonisamide do not appear to reduce efficacy

Answer 15

Progestin dose is lower than dose in COCs • Norethindrone (Camila): continuously • Drospirenone (Slynd): 24 active/4 inert tablets • Norethindrone POP does not consistently suppress ovulation—approximately half of women ovulate • Drospirenone POP suppresses ovulation, antimineralcorticoid activity

Answer 16

Add progestin to MHT for women with uterus • Progestin is not indicated in women who have undergone hysterectomy • Progestin is not indicated in low-risk women on low dose vaginal estrogen

Answer 17

Cyclic regimen 5–10 mg oral daily • Continuous regimen 1.25–2.5 mg oral daily •Most studies of progestins have been witht his compound • Prevents endometrial hyperplasia • Associated with increase risk of breast cancer, possibly coronary heart disease, and unfavorable effect on lipids

Answer 18

``` Micronized progesterone • Cyclic regimen 200 mg oral daily • Continuous regimen 100 mg oral daily • Bioidentical • Commonly prescribed • Protects endometrium • Minimal negative effect on lipids • No apparent increase to risk of breast cancer or coronary heart disease ```

Answer 19

Natural progesterone (Prometrium) 200 mg daily oral: days one to 14 of each calendar month • Given with continuous daily estrogen • Majority of women have monthly withdrawal bleeding

Answer 20

Estrogen and progestin are usually given as separate pills • Induces amenorrhea in most women • Standard dose of estrogen • 17-beta estradiol 1 mg oral • Transdermal estradiol 0.05 mg • Standard dose of progestin • Natural progesterone (Prometrium) 100 mg daily oral

Answer 21

Oraloptions(progestinsderivedfrom testosterone) • Norethindrone • Norgestimate • Drospirenone (spironolactone derivative) • Transdermal options (17-beta estradiol combined with progestin • Norethindrone applied twice weekly • Levonorgestrel applied once weekly Levonorgestrel- releasing IUDs are not approved in U.S. for endometrial protection in menopausal women on estrogen, but are used off-label for women who cannot tolerate oral progestin. Adverse effects • Irregular bleeding • Bloating • Mood changes

Answer 22

Progesterone Antagonist Indication: termination of intrauterine pregnancy, Cushing syndrome • Risk of serious complications including bleeding and bacterial infections • Only available through restricted access program

Answer 23

``` Indications • Osteoporosis • High fracture risk • Hypercalcemia • Metastatic bone disease • Paget disease ``` Inhibit bone resorption by reducing osteoclast number and function Poorly absorbed orally • Best given on empty stomach with eight ounces water to enhance absorption and stay upright for at least 30 minutes • Potentially cause esophagitis/gastricirritation • Long half-life • Renally excreted: not recommended in moderate to severe kidney disease ``` Absolute contraindication • Uncorrected hypocalcemia • Delayed esophageal emptying (stricture, achalasia) • Inability to stand or sit upright for at least 30 minutes • Increased risk of aspiration • Avoid if CrCl under 35 • Caution if GI pathology ``` ``` Adverse effects • Atypical femur fractures • Severe bone/joint/muscle pain • Upper GI mucosa irritation (esophagitis, ulcers, dysphagia) • Hypocalcemia • Jaw osteonecrosis ``` Duration of therapy • If fracture risk remains high after initial five years, consider changing to alternative therapy or extending oral bisphosphonate for up to ten years • Consider drug holiday after initial five years of therapy if bone mineral density is stable • Optimal length of drug holiday is usually for up to five years

Answer 24

Bisphosphonates inhibits bone resorption without inhibiting bone formation • 35 mg oral once weekly • 150 mg oral once monthly

Answer 25

Bisphosphonates highly selective inhibitor of bone resorption • 70 mg oral once weekly

Answer 26

lack of evidence for prevention of hip or non-vertebral fracture

Answer 27

``` 5 mg IV once yearly • More risk of renal toxicity • Check creatinine before each dose • Push fluids before and after each dose • Acetaminophen after infusion may reduce acute- phase reaction (influenza-like) ``` treats high blood calcium

Answer 28

Xanthine Oxidase Inhibitors Chronic gout Pharmacodynamics • Decrease uric acid levels by selectively inhibiting xanthine oxidase, which is the enzyme responsible for the conversion of hypoxanthine to xanthine to uric acid. Uric acid then decreases, reducing the risk of crystallization and a gout attack Caution and contraindications • Caution in renal impairment • Avoid use with azathioprine, mercaptopurine, and theophylline • Avoid in severe hepatic dysfunction • Allopurinol may be used in children over six years old related to hyperuricemia from cancer therapy • Avoid in pregnancy and use allopurinol with caution in lactation Adverse drug effects • Maculopapular skin rash, arthralgias, nausea, diarrhea, elevated transaminases, hypersensitivity (rare), hepatotoxicity (rare)

Answer 29

Indications • Chronic gout Pharmacodynamics • Increases the excretion of serum uric acid by competitively inhibiting the reabsorption of uric acid at the proximal convoluted tubule Adverse drug effects • Headache, dizziness, anorexia, nausea and vomiting, gingival soreness, urinary frequency, dermatitis, pruritus, flushing fever, and gout exacerbation; anaphylaxis (rare), blood discrasias (rare) Caution and contraindications • Avoid in patients with diagnosed blood dyscrasias • Avoid use if CrCl is under 30 mL/minute • Avoid in children less than two years old • Avoid in combination with aspirin • Avoid in patients with G6PD deficiency • Avoid in pregnancy and lactation • Avoid with sulfa allergy

Answer 30

Indication • Acute gout flare Pharmacodynamics • Inhibits the activation, degranulation, and migration of neutrophils to the area of a gout attack. This then decreases the inflammation and pain associated with a gout attack ``` Caution and contraindications • Avoid in combination with grapefruit juice • Caution in renal impairment • Caution in hepatic impairment • Caution in elderly patients • Caution in pregnancy and lactation • May be used in pediatrics older than 16 for gout treatment ```

Answer 31

Corticosteroids Indications • Acute gout, rheumatoid arthritis • Pharmacodynamics • Decreases inflammation by suppressing migration of polymorphonuclear leukocytes (neutrophils, eosinophils, basophils) and reversing increased capillary permeability Caution and contraindications • Avoid in uncontrolled active infections • Prolonged use may lead to adrenal suppression and immunosuppression • Caution in diabetic patients and those with active GI disease • Caution in renal and hepatic impairment • Caution in pregnancy and lactation • Approved in pediatrics Adverse drug effects • Hypertension, insomnia, mood changes, increased appetite, glucose intolerance, peptic ulcer (cutaneous atrophy, cataracts, glaucoma, osteoporosis, growth suppression, Cushing’s syndrome with chronic use)

Answer 32

Indications • Mild to moderate OA Pharmacodynamics • Exerts its action on CNS and COX, which results in a decreased prostaglandin synthesis. Active as analgesic and antipyretic, but not anti-inflammatory ``` Caution and contraindications • Avoid in severe hepatic impairment and severe active liver disease • Discontinue if skin reaction develops • Compatible in pregnancy and lactation • Approved in pediatrics ``` Adverse drug effects • Skin rash, dizziness, hypersensitivity reactions (rare)

Answer 33

Nonsteroidal Anti-Inflammatory Drugs Indications • Mild to moderate OA, rheumatoid arthritis Pharmacodynamics • Exerts anti-inflammatory action by inhibiting the conversion of arachidonic acid to prostaglandin, prostacyclin, and thromboxanes, all of which are mediators of pain and inflammation Caution and contraindications • Caution in cardiovascular disease • Avoid in pregnancy • Compatible in lactation • Caution in elderly patients • Caution in renal and hepatic impairment • Avoid use if GFR under 30 mL/minute • Approved in pediatrics over 6 months old Adverse drug effects • Edema, dizziness, skin rash, GI disturbances, elevated transaminases, dyspepsia, hypertension, bleeding due to reversibly impacting platelet aggregation • Black box warning: increased risk for thrombotic events; serious gastrointestinal bleeding, ulcerations, and perforations

Answer 34

Consider when the pain associated with OA progresses past responsiveness to APAP and NSAIDs Pharmacodynamics • Mu opioid receptor agonist that when binds, ascending pain pathways are inhibited. Tramadol also inhibits the reuptake of serotonin and norepinephrine, which are also involved in the ascending pain pathway Caution and contraindications • Caution in patients with substance abuse history • Avoid in patients with history of seizures due to lowering of seizure threshold • Caution in renal and hepatic impairment • Caution in pediatrics • Caution in elderly • Caution using with other CNS depressants Adverse drug effects • Dizziness, nausea, drowsiness, sweating. Also has the potential, similar to other mu receptor agonists, to cause constipation, dependency, euphoria, and respiratory depression • Risk of serotonin syndrome when combined with other serotonergic agents

Answer 35

Disease Modifying Anti-rheumatic Drugs Pharmacodynamics • A folic acid antagonist; is thought to affect leukocyte suppression, decreasing the inflammation that results from immunologic by-products Adverse drug effects • Nausea, diarrhea, arthralgias, oral ulcers, alopecia, photosensitivity, skin rash, dizziness, increased serum transaminases Caution and contraindications • Avoid in pregnancy and lactation • Avoid in patients with blood dyscrasias • Caution in renal and hepatic impairment • Black box warning: risk of hepatotoxicity, renal impairment, pneumonitis, bone marrow suppression, gastrointestinal toxicity, active stomatitis, dermatology reactions, and opportunistic infections

Answer 36

Biologic DMARDS (TNF Inhibitors) Pharmacodynamics • These agents act by binding the circulating TNF-alpha, rendering it inactive. This then reduces the chemotactic effect of TNF-alpha by reducing IL-6 and CRP, resulting in reduced infiltration of inflammatory cells into the joint. Cell lysis also occurs Caution and contraindications • Caution in patients with new/recurrent infections • Update immunizations before initiating • Approved in pediatrics over two years old • Limited data in pregnancy and lactation Adverse drug effects • Injection site reactions, infusion reaction, infections, dizziness, headaches, nausea

Answer 37

Hydantoin Indications Tonic-clonic and partial complex seizures Pharmacodynamics • Inhibit and stabilize electrical discharges in the motor cortex of the brain by affecting the influx of sodium ions during generation of nerve impulses Caution and contraindications • Avoid in sinus bradycardia, second- and third-degree AV block, and Stocks-Adams syndrome (syncope with heart block) • Caution in hypotension and myocardial insufficiency • Caution in renal and hepatic impairment • Rebound status epilepticus can occur with sudden withdrawal • Narrow therapeutic range • Avoid in pregnancy and lactation • Approved in pediatrics • Caution in elderly Adverse drug effects • Agitation, ataxia, confusion, dizziness, drowsiness, headache, nystagmus, hypotension, tachycardia, nausea, vomiting, anorexia, altered taste, gingival hyperplasia, discolored urine, hypersensitivity reactions (rare), suicidal ideations (rare), blood dyscrasias (rare)

Answer 38

Indications • Focal and generalized onset seizures Pharmacodynamics • Exact MOA unclear but thought to affect the sodium channels, slowing influx of sodium in the cortical neurons and slowing the spread of abnormal activity Caution and contraindications • Black box warning: development of SJS and toxic epidermal necrolysis in Chinese patients • Black box warning: blood dyscrasias • Black box warning: dermatologic toxicity • Caution in renal and hepatic impairment • Avoid in pregnancy and lactation • Caution in elderly • Approved in pediatrics Adverse drug effects • Drowsiness, dizziness, ataxia, nausea, vomiting, skin rash, pruritus, constipation, tremor, behavior changes (rare), suicidal ideations (rare), multi-organ hypersensitivity reactions (rare), hepatotoxicity (rare)

Answer 39

Indications • Partial seizures, primary generalized tonic- clonic seizures Pharmacodynamics • Thought to affect voltage-sensitive sodium channels and inhibit presynaptic release of glutamate and aspartate in the neuron Caution and contraindications • Black box warning: serious skin reactions • Rebound status epilepticus can occur with sudden withdrawal • Caution in renal and hepatic impairment • Avoid in pregnancy and lactation • Approved in children older than 2 y/o Adverse drug effects • Dizziness, headache, GI upset, diplopia, ataxia, insomnia, skin rash, SI (rare), blood dyscrasia (rare), multi-organ hypersensitivity reactions (rare)

Answer 40

Indications • Partial seizures in adults Pharmacodynamics • Exact MOA unknown but it blocks voltage- dependent sodium and chloride channels Adverse drug effects • Somnolence, anorexia, dizziness, headache, agitation, memory difficulties, aplastic anemia (rare), agranulocytosis (rare) Caution and contraindications • Avoid if hypersensitivity to sulfonamides • Avoid with sulfa allergy • Rebound seizures can occur with sudden withdrawal • Caution in renal and hepatic impairment • Avoid in pregnancy and lactation • Approved for pediatrics older than 16 years old

Answer 41

Succinimides Indication • Absence seizures Pharmacodynamics • Decrease nerve impulses and transmission in the motor cortex Adverse drug effects • GI distress, sedation, ataxia, lethargy, headache, rash, pruritus, mood changes Caution and contraindications • May continue in pregnancy with close monitoring • Avoid in lactation • Rebound seizures can occur with sudden withdrawal • Caution in renal and hepatic impairment • Approved for pediatrics older than 3 y/o

Answer 42

Indications • Focal (partial) onset seizures, generalized onset seizures, focal onset impaired awareness and absence seizures Pharmacodynamics • Increases GABA availability, enhances the action of GABA, mimics its action at postsynaptic sites Adverse drug effects • Headache, drowsiness, dizziness, nausea, vomiting, tremor, visual disturbance, weight gain, behavioral changes, hypersensitivity reactions (rare), SI (rare), brain atrophy (rare) ``` Caution and contraindications • Black box warning: hepatotoxicity • Black box warning: severe pancreatitis • Avoid in pregnancy and lactation • Avoid in children younger than 2 y/o • Caution in elderly • Rebound seizures can occur with sudden withdrawal ```

Answer 43

Indications • Focal seizures Pharmacodynamics • Thought to be a GABA analogue that binds to unknown receptors in the brain Adverse drug effects • Dizziness, drowsiness, fatigue, ataxia, peripheral edema, abnormal thinking Caution and contraindications • Only if benefits outweigh risks in pregnancy and lactation • Avoid in children younger than 3 y/o • Caution in renal impairment • Caution in elderly • Caution in patients with substance abuse history • Rebound seizures can occur with sudden withdrawal

Answer 44

Indications • Focal seizures, primary generalized tonic- clonic seizures Pharmacodynamics • MOA unclear but may block sodium channels or potentiate GABA Adverse drug effects • Ataxia, paresthesia, dizziness, somnolence, difficulty concentrating, mood changes, weight loss Caution and contraindications • Avoid in pregnancy • Only if benefits outweigh risks in lactation • Avoid in children younger than three months old • Caution in renal and hepatic impairment • Caution in elderly • Rebound seizures can occur with sudden withdrawal

Answer 45

Indications • Focal onset seizures, generalized onset seizures Pharmacodynamics • MOA unclear but may inhibit burst firing without affecting normal neuronal excitability Adverse drug effects • Somnolence, dizziness, somnolence, nervousness, mood disturbances, SI (rare) Caution and contraindications • Caution in pregnancy • Avoid in lactation • Avoid in children younger than one month old • Caution in renal impairment • Caution in elderly • Rebound seizures can occur with sudden withdrawal

Answer 46

Dopamine Agonists Pharmacodynamics • Levodopa circulates in the plasma to the blood-brain barrier, where it crosses to be converted by enzymes to dopamine. • Carbidopa inhibits the peripheral plasma breakdown of levodopa, thereby increasing the availability of levodopa at the blood-brain barrier Caution and contraindications • Avoid with narrow angle glaucoma • Avoid in patients with major psychiatric disorders • Avoid in patients with malignant melanoma • Caution with patients who have cardiovascular disease • Caution in elderly • Risk of neuroleptic malignant syndrome if abruptly stopped Adverse drug effects • Orthostatic hypotension, somnolence, dizziness, headache, depression, nausea, constipation, dyskinesia, hypertension, insomnia, abnormal dreams, neuroleptic malignant syndrome (rare), peripheral neuropathy (rare)

Answer 47

Muscle Relaxants Pharmacodynamics • Inhibits the transmission of both monosynaptic and polysynaptic reflexes at the spinal cord level, possibly by hyperpolarization of primary afferent fiber terminals, which results in relief of muscle spasticity ``` Caution and contraindication Caution in renal impairment • Caution in elderly • Caution with seizure disorder • Avoid in pregnancy • Caution in lactation ``` Adverse drug effects • Drowsiness, confusion, headache, nausea, vomiting, hypotension, seizures

Answer 48

Pharmacodynamics • Act on the monosynaptic and polysynaptic spinal reflexes; inhibiting the synaptic reflex arcs affects the messages that are producing and maintaining the skeletal muscle spasm Adverse drug effects • Dry mouth, drowsiness, fatigue, nausea, vomiting, constipation, hallucinations, blurred vision Caution and contraindication • Avoid in hyperthyroidism, heart failure, arrhythmias, heart block or conduction disturbances and acute recovery phase of MI • Caution in patients with urinary retention, angle closure glaucoma or increased ocular pressure • Caution in hepatic impairment • Approved in pediatrics older than 12 years • Limited data in pregnancy and lactation

Answer 49

Pharmacodynamics • Centrally acting alpha-2 adrenergic agonist that reduces muscle spasticity by presynaptic inhibition of motor neurons Adverse drug effects • Dry mouth, weakness, fatigue, constipation, hypotension, bradycardia, hepatotoxicity (rare), anaphylaxis and angioedema (rare) ``` Caution and contraindications Avoid in hepatic impairment • Caution in renal impairment • Avoid alcohol use • Do not abruptly stop • Caution in elderly • Avoid in pregnancy and lactation • Should only be used by specialist in pediatrics ```

Answer 50

Cholinesterase Inhibitors Pharmacodynamics • Reversibly and noncompetitively inhibits centrally active acetylcholinesterase (AChE), which results in increase levels of acetylcholine available for synaptic transmission in the CNS Adverse drug effects • Dizziness, headache, agitation, falls, weight loss, nausea, vomiting, diarrhea, insomnia, tremor Caution and contraindications • Avoid in combination with anticholinergic drugs • Caution in renal and hepatic impairment • Caution with seizure disorder • Risk of QT prolongation (Donepezil)

Answer 51

NMDA Receptor Antagonist Pharmacodynamics • Low to moderate, noncompetitive antagonist at NMDA receptors; persistent stimulation of NMDA receptors by glutamate is thought to possibly contribute to the symptomatology of AD Adverse drug effects • Confusion, dizziness, constipation, headache, somnolence, hypertension, diarrhea, hypersensitivity reaction (rare) Caution and contraindications • Caution in cardiovascular disease • Caution in renal impairment • Caution with seizure disorder

Answer 52

Alpha-1 Selective Antagonists Pharmacodynamics • Hypertension: “competitively inhibits postsynaptic alpha-1 receptors which result in vasodilation of veins and arterioles and a decrease in total peripheral resistance and blood pressure” • BPH: competitively inhibits postsynaptic alpha-1 receptors in prostatic stromal and bladder neck tissues; this reduces the sympathetic tone-induced urethral stricture causing BPH symptoms Caution and contraindications • Caution in patients with heart failure, angina, or recent MI • Avoid “zosins” in the presence of volume depletion • Caution in renal and hepatic impairment • Caution in elderly- beer’s list medication • Limited data in pediatrics • Avoid in pregnancy and lactation Adverse drug effects • Fluid retention, nasal congestion, blurred vision, dry mouth, constipation, impotence, urinary frequency, headache, dizziness, fatigue, priapism (rare), allergic reactions (rare)

Answer 53

Alpha-2 Agonists: Central Indications • Hypertension,ADHD Pharmacodynamics • Hypertension: stimulates alpha-2 receptors in the brain stem, activating an inhibitory neuron, resulting in reduced sympathetic outflow from the CNS, decreasing peripheral resistance, heart rate, blood pressure and renal vascular resistance • ADHD: MOA unknown; thought that it regulates activity in the prefrontal cortex responsible for emotions, attention, and behaviors Caution and contraindications • Do not stop abruptly • Caution with severe coronary insufficiency • Avoid in those at risk or with history of bradycardia • Caution in renal impairment • Caution in cerebrovascular disease • Caution in pregnancy • Avoid in lactation • Caution in elderly- beer’s list medication • Approved for pediatrics Adverse drug effects • Drowsiness, headache, fatigue, dizziness, skin rash, xerostomia, bradycardia, nightmares, constipation, impotence

Answer 54

Indications: HTN Pharmacodynamics • Stimulation of central alpha-2 receptors by methyldopa’s metabolite alpha-methylnorepinephrine produces a decrease in sympathetic outflow to the heart, kidneys, and blood vessels ``` Caution and contraindications • Caution with severe coronary insufficiency • Avoid in those at risk or with history of bradycardia • Caution in renal impairment • Avoid in active liver disease • Caution in cerebrovascular disease • Compatible with pregnancy • Avoid in lactation • Caution in elderly • No longer recommended in pediatrics ``` Adverse drug effects • Edema, sedation, bradycardia, hypotension, skin rash, myalgia, elevated LFTs, hemolytic anemia (rare), hepatotoxicity (rare)

Answer 55

Selective Beta Blockers Indications • Heart failure, hypertension, atrial fibrillation, angina, treatment post-acute MI Pharmacodynamics • Block beta-1 receptors at the SA node to decrease heart rate, decrease contractility in the atria and ventricles and conduction velocity, and slow conduction at the AV node Caution and contraindications • Do not abruptly withdraw • Avoid in patients with bronchospasms • Avoid in patients with second- or third-degree AV block • Caution in peripheral vascular disease • Caution in diabetic patients • Caution in hyperlipidemia • Other agents preferred in pregnancy and lactation • Other agents preferred in pediatrics for hypertension • Caution in elderly Adverse drug effects • Hypotension (including orthostatic), bradycardia, dizziness, drowsiness, fatigue, insomnia, depression, pruritus, impotence, decreased libido, anaphylactic reactions (rare)

Answer 56

Nonselective Beta Blockers Indications • Atrial fibrillation, essential tremor, migraine prophylaxis, hypertension, stable angina, thyroid storm Pharmacodynamics • Competitively block response to beta-1 and beta-2 stimulation, which results in decreased heart rate, myocardial contractility, BP, and myocardial oxygen demand ``` Caution and contraindications • Do not abruptly withdraw • Avoid in patients with bronchospasms • Avoid in patients with second or third-degree AV block • Caution in peripheral vascular disease • Caution in diabetic patients • Caution in hyperlipidemia • Other agents preferred in pregnancy and lactation • Approved in pediatrics • Caution in elderly ```

Answer 57

Indications • Hypertension, HF with reduced ejection fraction, left ventricular dysfunction following MI Pharmacodynamics • Nonselective beta receptor blockade and alpha-1 receptor blockade thereby decrease blood pressure and peripheral resistance; these combined effects decrease myocardial oxygen demand and lower cardiac workload Caution and contraindications • Do not abruptly withdraw • Avoid in patients with bronchospasms • Avoid in severe hepatic impairment • Avoid in patients with second- or third-degree AV block • Avoid in patients with NYHA Class IV HF • Caution in peripheral vascular disease • Caution in diabetic patients • Caution in hyperlipidemia • Other agents preferred in pregnancy and lactation • Initiated by cardiologist in pediatrics Adverse drug effects • Hypotension (including orthostatic), dizziness, fatigue, weight gain, hyperglycemia, headache, nausea, vomiting, impotence, anaphylactic reactions (rare)

Answer 58

Indications: • Hypertension including severe acute Pharmacodynamics • Nonselective beta receptor blockade and alpha-1 receptor blockade thereby decrease blood pressure and peripheral resistance; these combined effects decrease myocardial oxygen demand and lower cardiac workload ``` Caution and contraindications • Do not abruptly withdraw • Avoid in patients with bronchospasms • Avoid in severe liver impairment • Avoid in patients with second- or third-degree AV block • Avoid in patients with NYHA Class IV HF • Caution in peripheral vascular disease • Caution in diabetic patients • Caution in hyperlipidemia • Compatible in pregnancy after first trimester • Caution in lactation • Limited data available in pediatrics ```

Answer 59

Indications • Emergency treatment of type 1 allergic reaction, including anaphylaxis Pharmacodynamics • Decreases the vasodilation and vascular permeability that occur during anaphylaxis; it relaxes smooth muscles, relieves bronchospasm, wheezing, dyspnea, pruritus, angioedema, and urticaria Caution and contraindications • Caution in cardiac disease • Compatible in pregnancy and lactation • Approved in pediatrics • Adverse drug effects • Apprehensiveness, tremor, anxiety, weakness, headache, palpitations, angina, alterations in blood sugar, disorientation, hypertension

Answer 60

Fluoxetine, sertraline, citalopram, escitalopram, paroxetine, fluvoxamine All the SSRIs affect the serotonin NT in the synaptic cleft by blocking the serotonin transporter from returning remaining serotonin to the presynaptic cell. • Through this mechanism, more serotonin is available to bind with the postsynaptic receptors. • Although, traditionally, these drugs are referred to as selective serotonin reuptake inhibitors, each one has different effects on other neurotransmitters. • For example, fluoxetine significantly affects dopamine that contributes to the development of side effects. • Citalopram and escitalopram are probably the closest to a true selective serotonin reuptake inhibitor. Side effects: Nausea, vomiting, diarrhea, agitation, insomnia, sexual side effects, serotonin syndrome, increased risk for upper gastrointestinal bleeding, and hyponatremia; QTc prolongation with citalopram All are taken orally and absorbed in the GI tract. • Absorption is largely unaffected by food. • Peak plasma levels range from 3–11 hours. Significant first pass effect: liver • Metabolized mostly by the CYP 450 system • Excreted: kidneys Half-life varies: 16–144 hours • Withdrawal symptoms are related to half-life • Half-lives can be shorter in children—increased risk of withdrawal • Prozac (fluoxetine) has the longest half-life, 96–144 hours, with chronic use and the fewest withdrawals Precautions • Suicidality: increase suicidality risk in children, adolescents, and young adults • Monitor for clinical worsening, unusual behavior changes, and advise family/caregivers to give close observation • Contraindications • Hypersensitivity to SSRIs • Received MAOI in past two weeks • Severe hepatic or renal insufficiency ``` Depressive disorders • Anxietydisorders • Panic disorders • OCD • Body dysmorphic disorder • Bulimia • Premenstrual dysphoric disorder • PTSD • Vasomotor symptoms of menopause ``` Data on SSRI usage during pregnancy do not support significant teratogenic risks

Answer 61

Vilazodone

Answer 62

Venlafaxine (Effexor) • MDD, PTSD, GAD, social anxiety, panic disorder Desvenlafaxine (Pristiq) • MDD, vasomotor symptoms, fibromyalgia, GAD, social anxiety, panic disorder, PTSD, postmenstrual dysphoric disorder Duloxetine (Cymbalta) • MDD, diabetic peripheral neuropathy, fibromyalgia, GAD (seven years and older), chronic musculoskeletal pain, stress urinary incontinence, neuropathic pain/chronic pain, other anxiety disorders Levomilnacipran (Fetzima) • MDD, fibromyalgia, neuropathic pain/chronic pain Milnacipran (Savella) • Only approved in the United States for fibromyalgia SNRIs may be effective in treating depression in patients whom SSRIs are ineffective Side effects: Nausea, vomiting, diarrhea, agitation, insomnia, sexual side effects, serotonin syndrome, increased risk for upper gastrointestinal bleeding, and hyponatremia; QTc prolongation with citalopram Noradrenergic side effects of tachycardia, dry mouth, diaphoresis, constipation

Answer 63

Amitriptyline, nortriptyline, imipramine, doxepin, desipramine May be associated with: Cardiovascular disease, arrhythmias, orthostatic hypotension, anticholinergic side effects (dry mouth, blurred vision, constipation, urinary hesitancy, memory impairment, confusion), sedation highly cardiotoxic; fatal in OD; secondary to life-threatening arrhythmias; narrow therapeutic index (e.g., five or six times maximum daily dose of imipramine can be lethal); weight gain is common; orthostatic hypotension

Answer 64

Buproprion, mirtazapine, nefazodone, trazodone, vortioxetine

Answer 65

Monoamine oxidase inhibitors Side effects: Hypertensive crisis, orthostatic hypertension, serotonin syndrome 2% of psychiatric prescribers use these; interact with tyramine (found in many foods) to cause hypertensive crisis; dangerous in OD; drug-to-drug interactions and require washout period from other medications

Answer 66

least likely to cause weight gain; can be activating; long half-life

Answer 67

interacts with a lot of other medications; nasty withdrawal; weight gain; sedating

Answer 68

BB warning QTc prolongation (maximum dose 40 mg daily; 20 mg daily if over 60 years old)

Answer 69

tends to be weight-neutral and neither sedating nor activating

Answer 70

monitor HR and BP (increases are dose-dependent)

Answer 71

low dose causes sedation (15 mg, take 0.5 tab at half strength), as does increased sedative factor diminishes

Answer 72

avoid in seizure-risk patients; avoid in those with anxiety; may be helpful for ADHD; Eeyore depression

Answer 73

Initial improvement may be seen in one to two weeks, but typically, for the maximum improvement ranges, from four to 12 weeks are required. • If no response is seen in four to eight weeks with the maximally tolerated dose: • Switch to a different antidepressant within the same or different class After complete remission of symptoms: • Antidepressant therapy should continue for at least four to nine months • Individuals who have had three or more episodes of depression most likely will need continuous maintenance therapy.

Answer 74

Can be life-threatening Cause • Taking more than one serotonin-related medication (prescription and CAM: St. John’s wart, grapefruit, ergot, woodrose, SAMe, cesium, lithium (Natural Medicines, 2016) Symptoms • Autonomic instability (breathing and BP), restlessness, agitation, myoclonus (sudden, involuntary jerking of a muscle or group of muscles), hyperreflexia (overactive or overresponsive reflexes), hyperthermia, diaphoresis, altered sensorium, tremor, chills, diarrhea and cramps, ataxia (loss of full control of bodily movements), headache, insomnia Treatment • DC SSRI; muscle relaxants; serotonin-blocking agents; O2; IV fluids; medications to control BP and HR; a breathing tube and medication to paralyze your muscles Course • Milder cases resolve in 24–72 hours • Moderate to severe cases can take weeks

Exam 3 Meds Flashcards

(98 cards)