Pharm Exam 2--opioids, anticonvulsants, NSAID, DMARD Flashcards

Question

Bupivicaine (Marcaine)

Answer 1

AMIDE - long DoA - **sensory before motor (more sensory than motor) - infiltration, spinal anesthesia, ***epidural - post-op pain control - **greater cardiotoxicity - -high affinity to resting cardiac Na channels - -reverse w/ lipids - -do NOT use for IV regional anesthesia

Answer 2

AMIDE - long DoA - rarely used for infiltrative, peripheral, or epidural blocks - **motor before (or w/o) sensory block - may cause inverse differential block

Answer 3

AMIDE - intermediate DoA - **Highest rate of clearance (careful w/ pts w/ liver damage) - metabolite may produce met-Hb - limited to dentistry due to met-Hb - do NOT use in pts w/ - -cardiac or respiratory disease - -idiopathic/congenital met-Hb-emia - reverse w/ methylene blue

Answer 4

ESTER - used in infiltration anesthesia & *diagnostic blocks - short DoA - potency of others are RELATIVE to Procaine - PABA metabolic product → ↓ action sulfonamide - minimal systemic toxicity - no local irritation - available w/ or w/o epi (2x DoA)

Answer 5

ESTER - *spinal anesthesia w/ dextrose (heavier than CSF) - used for ophthalmological - long DoA & slow onset of action - 16x more potent/toxic than procaine

Answer 6

AMIDE - infiltration & epidural anesthesia - intermediate DoA; potency of 4 - rapid onset, minimal local irritation - some topical activity - **Transient neurological symptoms (transient pain, dysesthesia) - -if used as spinal anesthesia (NOT DOC for spinal)

Answer 7

ESTER - topical anesthesia of mucous membranes around URT - short acting - topical only - ↑ catecholamine in CNS and periphery - -vasoconstriction NARCOTIC: - ↓ repuptake of DA (and NE) - energy burst, euphoria - stimulates SYMPATHETIC - -↑ HR, BP → cerebral hemorrhage - -mydriasis - -↓ appetite -hyperthermia, seizures

Answer 8

AMIDE - high volume peripheral blocks & epidural - S-enatiomer of bupivicaine - **less cardiac toxicity - **less lipid soluble & cleared more rapidly - -adverse effects less likely - PHK similar to bupivicaine - minor vasoconstricting

Answer 9

AMIDE - peripheral nerve blocks - NOT used in labor → toxic to neonate - intermediate DoA - potency 2

Answer 10

AMIDE - has additional ester group- esterases metabolize - -↓ half-life & systemic toxicity - widely used in dentistry - -large therapeutic window & low potential systemic toxic - -can inject more later - may devole persistent paresthesias

Answer 11

AMIDE - inhibits butyryl-AChase - Dibucaine numer shows activity of butyryl-AChease - differentiate b/w substitution mutations of butyryl-AChease - inhibits wild type (normal) MORE than mutated type

Answer 12

(use and mechanism) -Activates nicotinic receptors in CNS & periphery PERIPHERY --↑ Epi release --↑ HR, BP --↑ tone & activity of GI CNS --**↑ 5HT & DOPAMINE release (↑ DA → endogenous opioid) --effects memory and learning (nicotinic receptors) -induces CYP450 - psychological & physical dependence; withdrawal - -Buproprion ↓ craving (receptors up-regulated)

Answer 13

(effects and drawbacks w. chronic use, medical effects) - targets presynaptic cannabinoid receptor (CB1) to alter NTM release - inhibits ACh & glutamate release - -impairs memory & cognitive function of hippocampus HARMFUL EFFECTS: - amotivational syndrome - ↓ testoserone - depression, paranoia, panic MEDICAL EFFECTS - anti-emetic - analgesia

Answer 14

(mxn, effects, toxicity) - Blocks 5HT transporter (SERT) - ↑ 5HT release - ↑ postsnyaptic 5HT receptors (↑ 5HT all over brain) -causes feelings of peace, empathy, acceptance - neruotoxic due to SERT inhib - can cause confusion, depression, anxiety, insomnia etc - death due to dehydration, hyperthermia, heart, kidney failure

Answer 15

(basic mxn & effects) - Binds 5HT2 (Gq) - no effect on mesolimbic DA → no reinforcement/ dependence - profound CNS w/ minimal peripheral effects - euphoria - visual hallucinations, altered perceptions, synesthesia - labile mood (elation to fear) - Mescaline: peyote; less potent - Psilocybin: muschrooms

Answer 16

(basic mxn & effects) -developed as a dissociative anesthetic - Targets NMDA/glutamate system - stimulant - depressant - hallucinogenic - analgesic - physically aggressive behavior - amnesia or personality changes

Answer 17

(basic mxn & effects) - targets NMDA/glutamate - causes feelings of floating or dissociation - sympathomimetic

Answer 18

(basic mxn & effects) - targets GABA system; ↑ inhibition - effective in preventing memory storage

Answer 19

-blocks VMAT and reverses DAT → ↑ DA (NE) - **neurotoxic effect → damage DA-ergic & 5HT-ergic - causes loss of DAT - cardiac toxicity- pulm edema, heart failure - formication- bugs under skin - Dependence and Tolerance occur rapidly - Dilated pupils

Answer 20

- produce dizzines and intoxication - symptoms: burns on lips or chemical smell - Smooth muscle relaxants that cause euphoria - hypotension & reflex tachy - effects occur w/in 30 sec

Answer 21

NSAID (analgetic, antipyretic, antiinflammatory, anitplatelet) -irreversible inhibitor of both COX-1 & COX-2 - -analgetic: central & peripheral ↓ PG synthesis; prevents sens. of pain receptors - -antipyretic: acts at hypothalamic area ↓ fever & malaise - -antiinflammatory: ↓ PG; ↓ tissue damage - -antiplatelet: lack ability to make more COX; can't activate or cause others to activate (lasts 8-10 days) - readily absorbed in stomach; ↑ [ ] in mucosal cells - hydrolyzed in plasma, liver, erythrocytes - **binds plasma proteins (50-90%); cometes w/ other drugs that bind--WARFARIN - low dose → 1st order; high dose → 0 order - excreted by kidneys: alkalize urine ↑ excretion; - -↓ GFR ↓ excretion Adverse reactions: respiratory & metabolic, platelet, uric acid, lungs, GI tract, kidneys

Answer 22

(analgesic & antipyretic; NO anti-inflammatory) - -not effective anti-rheumatic - -equipotent to aspirin for anaglesia & antipyretic - not a COX inhibitor, preferred if patient has: - -allergic reaction to ASA - coagulation disorders (hemophilia) - peptic ulcers - gouty arthritis & taking uricosuric agents - metabolized by CYP2E1 in liver - -chronic et-OH can ↑ toxicity overdose causes FATAL HEPATIC NECROSIS - -caused by hydroxylated intermediate metabolite - -uses up Glutathione - -↑ serum transaminase, LDH - -progress to encephalopathy, coma, death Treat OD w/ - N-acetylcysteine (w/in 10-12 hrs) - gastric empty (w/in 4 hours) - forced diuresis - hemodialysis

Answer 23

NSAID (analgetic, antipyretic, antiinflammatory) - *very potent anti-inflam & anti-rheumatic - -**worst side-effect profile--GI irritation - inhibits phospholipase A2 - reduce PMN migration - used for patent ductus arteriosus primary NSAID used in Gout - acute attacks of Gout** + colchicine - -aspirin or salicylate CI in gout → ↓ excretion

Answer 24

NSAID (analgetic, antipyretic, antiinflammatory) - VERY potent - analgesic in post-surgical pain (instead of opioids that cause constipation) - oral, IV, IM - after 5 days of use → frequent GI SE

Answer 25

NSAID (analgetic, antipyretic, antiinflammatory) - potent COX inhibitor - mostly GI side effects - combine w/ misoprostol (PGE1 analog) → Arthrotec - -protects GI

Answer 26

NSAID (analgetic, antipyretic, antiinflammatory) best adverse effect profile - first choice drug - lowest incidence of side-effects - treatment of RA and OA - combo w/ ASA ↓ effect

Answer 27

NSAID (analgesic, antipyretic, antiinflammatory) - Longest lasting (fewest daily doses) - treat RA, OA, ankylosing spondylitis - extensively binds to *plasma proteins (anticoagulants, hypoglycemic agents) - MIGRAINE treatment

Answer 28

NSAID (analgetic, antipyretic, antiinflammatory) - inhibits PMN migration & lymphocyte function - ↓ oxygen radical production - long half-life - high incidence of GI SE

Answer 29

NSAID (analgetic, antipyretic, antiinflammatory) -pro-drug that must be converted to active metabolite

Answer 30

DMARD - Anti-muscarinic, anti-cholinesterase, anti-protease - inhibits PG synthesis - inhibits biosynthesis of mucopolysaccharide - inhibits responses to chemotactic stimuli & phagocytosis - stabilizes lysosomes - reacts w/ NA and tissue proteins -High affinity for melanin--concentrates in epidermis and retina - toxicity: hemolysis (G6PD def), NADPH synthesis is hindered and can't reduce met-Hb to Hb - ototoxicitym retinopathy, peripheral neruopathy

Answer 31

DMARD -metabolized to Mesalamine by intestinal bacteria Mesalamine -inhibits COX → inhibit AA metabolism -inhibits lipoxygenase → inhibits LT synthesis -was used to treat IBD toxicity: GI and Rash, - Hepatitis and Blood dycrasias are rare - -monitor hepatitis & marrow suppression for first 2-3 weeks

Answer 32

DMARD--acts on TNF-α - Chimeric IgG1k MAb against TNF-α - treatment of Crohns & RA - -combined w/ methotrexate in RA General Adverse effect themes: 1) Injection: irritation & pain 2) CI in children & pregnancy: don't know effects yet 3) Immunosuppresion: ↑ risk of infections & cancer - Hypersensativity: murine protein ↑ chance

Answer 33

DMARD--acts on TNF-α - Recombinant human IgG1 MAB - unlike Infliximab, approved for MONOTHERAPY in RA General Adverse effect themes: 1) Injection: irritation & pain 2) CI in children & pregnancy: don't know effects yet 3) Immunosuppresion: ↑ risk of infections & cancer - Hypersensativity: murine protein ↑ chance

Answer 34

DMARD--acts on TNF-α -Humanized Ab that is POTENT neutralizer of TNF-α General Adverse effect themes: 1) Injection: irritation & pain 2) CI in children & pregnancy: don't know effects yet 3) Immunosuppresion: ↑ risk of infections & cancer - Hypersensativity: murine protein ↑ chance

Answer 35

DMARD--acts on TNF-α -Human derived MAb against TNF-α General Adverse effect themes: 1) Injection: irritation & pain 2) CI in children & pregnancy: don't know effects yet 3) Immunosuppresion: ↑ risk of infections & cancer - Hypersensativity: murine protein ↑ chance

Answer 36

DMARD--acts on TNF-α - dimeric fusion protein-- fake TNF-α receptor - -NOT a MAb - Binds and inactivates TNFα - doesn't affect TNF production or serum levels General Adverse effect themes: 1) Injection: irritation & pain 2) CI in children & pregnancy: don't know effects yet 3) Immunosuppresion: ↑ risk of infections & cancer - Hypersensativity: murine protein ↑ chance

Answer 37

DMARD--inhibitor of NA synthesis -↓ immune reaction -inhibits de novo PYRIMIDINE synthesis via → inhibit dihyroorotate dehydrogenase (DHODH) -inhibits tyrosine kinase associated w/ cytokine and GF receptor -inhibits induction of COX-2 -ORAL administation

Answer 38

DMARD--inhibitor of NA synthesis -↓ immune reaction -inhibits lymphocyte PURINE synthesis → inhibits inosine monophosphate dehydrogenase - ORAL administration - prodrug for mycophenolic acid (MPA)

Answer 39

DMARD--interleukin receptor antagonist - recombinant IL-1 receptor antagonist (IL-1Ra) - improves swollen and painful joints

Answer 40

DMARD--interleukin receptor antagonist - humanized MAb that inhibits IL-6 receptor - Adverse reaction similar to other immunosuppressants

Answer 41

DMARD--JAK inhibitor - primarily inhibits JAK1, JAK3, and some JAK2 - may precipitate SERIOUS INFECTIONS and MALIGNANCY

Answer 42

DMARD - Chelating agent effective in RA (and in Wilson's disease) - inhibits collagen formation - ↓ CIRCULATING IgM rheumatoid factor but not absolute lvls - depresses T-cell activity but NOT B-cell High incidence of adverse reactions: - thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia - AI diseases: SLE-like, pemphigus, Goodpasture, Myasthenia graves, polymyositis, stenosing alveoli's - alteration in TASTE - ↑ risk in pts >65

Answer 43

lipoxygenase inhibitor LT receptor inhibitor -effective against asthma

Answer 44

- 1st line treatment of glaucoma - ↑ resorption of aqueous humor - changes color of light blue eyes - PGF2α

Answer 45

- reversible inhibition of COX-2 (PGI2) - ↓ potential for gastropathy & GI bleed - ↑ risk of CVD due to ↑ ratio of TXA2 → vasoconstriction and platelet activation CI: GI disease, asthma, pregnancy, renal failure, sulfonamide hsn.

Answer 46

-combo of diclofenac & misoprostol Diclofenac-NSAID Misoprostol- PGE1 analog- protects GI

Answer 47

DMARD- inhibitor of B-cell diff - chimeric MAb against CD20 on pre-B & mature B-cell (>90% B-cell NHL) - CD20 NOT found on: hematopoietic SC, pro B-celll, normal plasma cell, or other normal tissue General Adverse effect themes: 1) Injection: irritation & pain 2) CI in children & pregnancy: don't know effects yet 3) Immunosuppresion: ↑ risk of infections & cancer - Hypersensativity: murine protein ↑ chance

Answer 48

DMARD- inhibitor T-cell activation & B-cell diff. - fully human recombinant fusion protein - costimulatory or 2nd signal BLOCKER of T-cell activation - -↓ host defense against infections and malignancies

Answer 49

- Initially ↑ respiration → respiratory alkalosis, - then ↓ respiration → metabolic & respiratory acidosis Warfarin + ASA: 1) inhibits platelet aggregation/coagulation (8-10 days) 2) displaces warfarin for PP-- 2% change = 2x [ ] Uric acid: ASA competes w/ reabsorption - ↓ excretion of UA & ↑ blood [ ]; exacerbates gout - very high [ ] ↓ UA secretion Lungs: blocks PG pathway which ↑ LT pathway → asthma GI tract: ↑ acid production → ulceration & bleeding -salicylates ↓ secretion of protective mucus Kidneys: ↓ PG allows ↑ vasoconstriction (ATII, NE, ADH) -renal damage, failure; interstitial nephritis, nephrotic syndrome Salicylism: (large repeated doses) dizziness, ringing ears, visual & hearing problems. Maybe skin eruptions, CNS problems Reye's syndrome: cerebral edema in children w/ viral infections (uncouples oxidative phosphrylation in hepatic mitochondria) Contraindications - Dont take aspirin for ~week before pregnancy or elective surgery - ↓ dose w/ oral anticoagulants, hypoglycemic agents - bleeding condition

Answer 50

- GI - pain, bleeding, ulcer, pancreatitis, diarrhea - CNS - headache, dizziness, confusion, depression - Lung - bronchoconstriction - Bone marrow - agranulocytosis, aplastic anemia - Nephrotoxicity - acute renal failure, interstitial nephritis, nephrotic syndrome - Hepatotoxicity - enzyme elevation, hepatitis - Hypersensitivity reactions

Answer 51

NSAID (analgetic, antipyretic, antiinflammatory) - less nephrotoxic - SEVERE GI effects including pancreatitis

Answer 52

DMARD -inhibit phagocytosis, proteolytic enzymes of PMN TOXICITY: bone marrow damage

Answer 53

Acute attack of Gout - inhibits phagocytosis of urate by PMN - -binds tubulin→ inhibits microtubular assembly - -helps terminate inflammatory process of ACUTE attack - inhibits formation of LTB4 - -inhibits leukocyte migration - effective only against gouty arthritis - no effect on rate excretion - no analgesic effect, no effect on COX - SE: **DIARRHEA. nausea, vomiting, abdominal pain - combine w/ indomethacin?

Answer 54

Hyperuricemia- uricosuric agent - reduces pool of uric acid by ↓ re-uptake in kidney (blocks organic anion transporter) - -prevent crystal formation and acute attack - wait 2-3 weeks after acute attack - **decreases excretion of many acidic compounds: - -*penicillin, NSAIDs glucuronides --should NOT be used in acute attack → ineffective & may precipitate an attack

Answer 55

Hyperuricemia- Xanthine oxidase inhibitor - decreases the formation of uric acid - -blocks metabolism of xanthine and hypoxanthine - metabolized by liver → oxipurinol (active compound) SE: vasculitis, agranulocytosis, hsn rxn -initially may provoke attack-- prophylaxis w/ colchicine DRUG INTERACTIONS: - ↑ effect of chemo mercaptopurines 6MP and azathioprine - ↓ activation of fluorouracil 5FU → ↓ effect - ↓ metabolism of Warfarin & Probenecid -should NOT be used in acute attack → ineffective & may precipitate an attack

Answer 56

Hyperuricemia- Xanthine oxidase inhibitor

Answer 57

Hyperuricemia- enzyme converting uric acid to *allantoin - recombinant form of urate oxidase (humans lack) - -allantoin is readily excreted - b/c it is a non-human protein HSN run occur - -can probably only use drug once

Answer 58

5-HT agonists- migraine symptoms - constricts mostly the large intracranial arteries - -highly selective for 5HT-*D receptors-- on intracranial vessels (AV anastomoses) - may ↓ release of neuropeptide-mediated inflammatory substance -NOT an analgesic-- direct vasoconstriction ↓ pain SE: VASOSPASM- coronary aa.(angina, MI), peripheral ischemia -rare cardiac arrhythmias--vent tachy/fib, arrest, death) CI: any vascular disease, renal impairment, breast feeding, HTN

Answer 59

5-HT agonists- migraine symptoms -causes vasoconstriction like -triptans , but less specific - partial agonist at 5-HT receptors in certain blood vessels - partial agonist at α1 - -antagonist of 5-HT in SM - -poor agonist/antagonist in CNS - more potent vasoconstrictor than -triptans - ergotism: vasoconstriction + CNS -pts w/ peripheral vascular disease should avoid

Answer 60

``` Valproic Acid: block Na channels, ↑ GABA, ↓ NMDA Topiramate: block Na channels, ↑ GABA, ↓ NMDA Botox ATII receptor blocker (-sartans) Β-blocker- Propranolol Clonidine CCB- Verapamil Antidepressants- Amitriptyline ```

Answer 61

Inhaled general anesthetic (properties & toxicities) -blocks NMDA - reduces hypotension** - little respiratory depression - Fast onset and recovery - second gas effect**→ ↑ rate of induction - **GOOD ANALGESIA (cannot produce anesthesia) - no renal or liver toxicity - diffusion hypoxia - replaces any trapped gas (nitrogen) → expands - -Caution occluded middle ear/eustacian tube, pneumothorax, loop of intestine, lung or renal cysts - DO NOT USE after EYE SURGERY (3 months) → irreversible loss of vision -**neurophathy w/ chronic exposure -inactivates Methionine synthase → ↓ DNA syntheses → ↓ WBC and RBC megaloblastic anemia

Answer 62

Inhaled general anesthetic (toxicities) -slow induction rapid awakening * *-Immune response (Cl- & Br-), * *-hepatitis (Cl- & Br-) * *-malignant hyperthermia (w/ succinylcholine) * *-cardiovascular problems- ↓ CO and arrhythmia * *-miscarriage - significant uterine relaxation (prolong delivery - ↓ renal function and urine flow - **depresses myocardium → ↓ CO - **sensitization to catecholamines → arrhythmias**

Answer 63

Inhaled general anesthetic (advantages/popularity) * *-MOST COMMONLY USED * *-HEPATIC and RENAL toxicity NONEXISTANT * *-useful in neurosurgery * *-low toxicity MAC 1.17 blood/gas 1.46 - induction & emergence > halothane or enflurane - vasodilation - ↓ BP (↓ w/ NOs), ↓ respiration - **↑ HR (prevent w/ opioids) * *-pungent odor -high [ ] → uterine relaxation -dilates cerebral vasculature → ↑ pressure -↓ cerebral metabolic 02 use → neurosurgery (Propofol ↓ BF) - does NOT depress myocardium or sensitize to catecholamines (Halothane) - vasodilation could cause coronary steal

Answer 64

Inhaled general anesthetic (advantage/popularity) MAC 1.80 blood/gas 0.69 (low solubility = easy control) * *-SAFEST drug for cardiovascular disease * *-LEAST respiratory irritation - **cardiac and respiratory depression minimal - least irritating, minimal odor → induction - -used in CHILDREN - rapid effect (0.69) - ↑ cerebral blood flow (prevent w. hyperventilation) - metabolized to Fl- → kidney damage (rare) - Compound A → kidney (degradation in machine)

Answer 65

Inhaled general anesthetic MAC 6.60 blood/gas 0.42 - Rapid EMERGENCE * *-pungent odor, irritates airways - similar circulatory effects as Isoflurane - -↓ BP, ↑ HR - ↓↓↓ respiration (& Propofol)

Answer 66

IV general anesthetic-- Barbituate - INDUCTION & short procedures not involving severe pain - -NO analgesic activity - ↓ cerebral O2 requirement → used w/ head trauma - heart and respiratory depression possible - CI in PORPHYRIA (↑ porphyrin synthesis)

Answer 67

IV general anesthetic--bezodiazepine - Sedation, anxiety relief, anterograde amnesia - pre-anesthetic and induction (given IV) - minor surgies w/ fentanyl - reverse with flumazenil -highly lipid soluble (rapid onset & short DoA)

Answer 68

IV general anesthetic (effects, uses, SE, advantages) DOC for most anesthetic procedures - -**induces as rapid as thipental - -**emergence is 10x faster - used for induction and maintenance - used in critical care settings - available as emulsion w/ albumin → **allergic reactions - -painful when injected (prodrug fospropofol ↓ pain) - SEVERE respiratory depressant (must monitor) - vasodilation but blunts baroreflex (no ↑ in HR) - -made worse by opioids - **least likely to cause nausea & vomiting - **↓ cerebral blood flow metabolism * IC pressure (neurosurgery) (isoflurane ↑ blood flow) - safe in pregancny - Propofol infusion syndrome: young puts w/ head trauma - metabolic acidosis, hyperlipidemia, rhabdomyolysis, enlarged liver -facilitates action of GABA at GABAa highly lipid soluble (rapid onset & short DoA)

Answer 69

IV general anesthetic -MAIN USE- anesthesia in patients at risk of HYPOTENSION - facilitates action of GABA by ↑ available receptors - -may disperse endogenous inhibitors - half life constant - likely to cause vomiting and cause - ↓ seizure threshold - hiccups

Answer 70

IV general anesthetic - blocks NMDA receptors - catatonic state: no response to noxious stimuli, eyes open, respiration maintained - Dissociative anesthesia: profound analgesia and superficial level of sleep - LITTLE respiratory depression-- bronchodilation - Sympathomimetic: ↑ HR and BP - no nausea or vomitting - Emergence delirum: bizzare dreams, hallucinations, psychosis - ↓ w/ benzos - ↑ cerebral blood flow and intracranial pressure

Answer 71

EFFECTS of GENERAL ANESTHETICS -amnesia, analgesia, unconsciousness, ↓ autonomic response, immobility in response to pain - ↓ BP & HR: vasodilation, cardiac depression, ↓ baroreflexes, ↓ SNS tone - ↓ respiratory drive (gag, cough, LES) - ↓ metabolism in brain - ↑ intracranial pressure: ↑ blood flow from vasodilation - hypothermia - nausea & vomiting (relived 5ht3 agonist ondansetron) - HTN & tachy on emergence

Answer 72

Inhaled general anesthetic (JUST KNOW NAME) MAC 1.63 blood/gas 1.90 - more rapid induction than halo thane - muscle relaxation and analgesia - depress respiration - uterine relaxation -may produce fluoride → reversible kidney damage (rare)

Answer 73

``` Procaine 1 Short Cocaine 2 Med Mepivicaine 2 Med Lidocaine 4 Med (Prilocaine) Tetracaine 16 Long Bupivicaine 16 Long Ropivicaine 16 Long Etidocaine ```