Uiuc M2 2010 Pharmacology Exam 5

Front 1

Acetylcholine

Back 1

Foo

Front 2

Alcohol

Back 2

Mx: Sedative-hypnotic.
Fx: GABA-enhancer, NMDA-antagonist, 5HT/ACh modulator.
Tol: Rapid, few drinks (↑sedating dose, n/c lethal dose - ↓therapeutic index). X-tol: sedative-hypnotics, not to opioids.
W/D: Craving, tremor, irritability, nausea, sweating, sleep dist, tachycardia, HTN, perceptual distortion, seizures. Depends on daily dose. Tx by ethanol ingestion. Naltrexone for chronic alcoholism.

Front 3

Amphetamine

Back 3

Mx: NE+DA releaser, reuptake inhibitor, MAO inhibitor
Fx: Central: ↑attentiveness, ↑motor task performance, anorexia, ↑locomotor/speech activity, ↑insomnia. Periph: NE-like, ↑BP, ↑arrhythmias/anigna, ↑urinary sphincter tone, mydriasis, ↑GI activity (cramps, diarrhea, vomiting).
Tx: Narcolepsy, ADD
Tol: ↑↑↑psych dependence (DA reward mx). Rapid tolerance to most fx.
W/D: Exhaustion, depression, ↑appetite.
O/D: High dose: confusion, illusions, panic, suicidal/homicidal. V. high: psychosis (formication - tx chlorpromazine), vomiting, convulsions, coma.

Front 4

Atracurium

Back 4

Mx: Non-depolarizing NMB.
Fx: Competitive antagonist @ nicotinic receptor. Higher doses may block receptor. Sensitivity: face > eye > fingers > limbs/neck/trunk > intercostals/diaphragm. No CNS fx. Cardiac: low dose ↑HR, high dose ↓CO (histamine, ganglionic). ↓BP b/c histamine - pre-tx w/antihistamine.
ToxTx: Neostigmine.
Tx: Anesthesia adjunct, muscle relaxant, etc.
C/I: Asthma (histamine!), myasthenia gravis.
D/I: Local anesthetics may potentiate.
Specifics: No autonomic ganglia block, no cardiac muscarinic fx, slight histamine release. Intermediate duration, 1.5x potency.

Front 5

Atropine

Back 5

Foo

Front 6

Baclofen

Back 6

Mx: Spasmolytic
Fx: GABA-B agonist (↑K⁺ postsyn, ↓Ca²⁺ presyn)
Tx: Spinal cord dz/MS spasticity (not cerebral palsy)
S/E: CNS (crosses BBB) - confusion, ataxia, drowsiness, more seizures, hallucinations if fast withdrawal, ↓RR, coma.

Front 7

Benzodiazepine

Back 7

Foo

Front 8

Bupivacaine

Back 8

Mx: Amide local anesthetic
Fx: Na⁺ blocker, sensory > motor.
Tx: Labor/postop analgesia, injection/topical.
S/E: Cardiac > lidocaine, ↓dromotrope, ↓inotrope, severe v-arrhythmias.
Kx: Potency > lidocaine, very long acting (many days, longest acting topical)

Front 9

Carbamezapine

Back 9

Mx: Na⁺ blocker.
Fx: Reduce excitability, high frequency discharge, presynaptic transmitter release, potentiate postsynaptic GABA activity.
Tx: Partial seizures, tonic-clonic seizures: 1st choice. Also, manic-depressives.
Kx: PO slow, peak plasma 8hr, P450 metab.
S/E: Ataxia, diplopia (short), drowsiness/vertigo, ↓RR, nausea/vomiting, stupor, coma, aplastic anemia, agranulocytosis, liver tox.

Front 10

Chlorpromazine

Back 10

Tx: Psychosis w/amphetamine/methamphetamine
D/I: ↑depressant fx w/opioids.

Front 11

Clomiphene

Back 11

Mx: Weird pro-fertility (Anti-estrogen/contraceptive in non-humans)
Fx: Enlargement of ovaries, ↑gonadotropins (amplitude, not freq), anti-estrogenic fx (hot flashes). Blocks feedback @ hypothalamus + pituitary for fx: need intact HP axis.
Struct: Tamoxifen-ish.
Tx: Infertility: give on d5-10 of cycle, 70% ovulate, 30% conceive
S/E: Multiple births (8%), ovarian cysts (5-10%)

Front 12

Cocaine

Back 12

Mx: Ester local anesthetic
Fx: Na⁺ blocker, sympathomimetic, NE+EPI, DA, 5HT reuptake inhibitor
Tx: Legal: Topical-only (opthalmic→sloughing cornea).
S/E: Stimulant, euphoria/dysphoria, motor activity alteration, vomiting, medullary stim→depress (resp failure), arrhythmia, MI, HF.
Kx: Well absorbed, rapidly degraded by plasma esterase
Illegal: Euphoria, ↑motor, psychosis, ↑sympathetic.
Tol: Some cross b/w amphetamines. ↑↑↑psych dependence (DA reward mx).
W/D: Minor. Exhaustion, hypersomnia, depression, ↑appetite.
O/D: Seizures (tx diazepam), anxiety, paranoia (tx haloperidol), arrhythmias (tx lidocaine?).

Front 13

Codeine

Back 13

Mx: Opioid analgesic
Fx: Partial mu-Opioid agonist.
Tx: Analgesia (combined w/others), anti-tussive.
Kx: P450 (active metabs w/increased activity).
Else: See morphine.

Front 14

Dantrolene

Back 14

Mx: Spasmolytic
Fx: ↓Ca²⁺ @ sarcoplasmic reticulum (ryanodine receptor block).
Tx: Malignant hyperthermia, cerebral palsy spasticity, some MS (constant slow writhing), some para/quads.
S/E: Weakness, hepatox, diarrhea.

Front 15

Dextromethorphan

Back 15

Mx: Opioid
Fx: Mixed receptor agonist; no analgesia/addictiveness.
Tx: Anti-tussive.
Else: See morphine.

Front 16

Diazepam

Back 16

Mx: GABA enhancer.
Tx: Acute status epilepticus.
S/E: Sedation, respiratory/cardiac depression.
Tolerance: weeks-months. Alteration in GABA receptor. X-tolerance with barbiturates.
W/D: Ethanol-like. Tx w/long-lasting agents and taper.
ToxTx: Flumazenil.

Front 17

Dibucaine

Back 17

Mx: Amide local anesthetic
Fx: Na⁺ blocker
Tx: US: Topical, skin-only. Outside: spinal.

Front 18

Dopamine

Back 18

Foo

Front 19

Doxacurium

Back 19

Mx: Non-depolarizing NMB.
Fx: Competitive antagonist @ nicotinic receptor. Higher doses may block receptor. Sensitivity: face > eye > fingers > limbs/neck/trunk > intercostals/diaphragm. No CNS fx. Cardiac: low dose ↑HR, high dose ↓CO (histamine, ganglionic). ↓BP b/c histamine - pre-tx w/antihistamine.
ToxTx: Neostigmine.
Tx: Anesthesia adjunct, muscle relaxant, etc.
C/I: Asthma (histamine!), myasthenia gravis.
D/I: Local anesthetics may potentiate.
Specifics: No autonomic ganglia block, no cardiac muscarinic fx, slight histamine release. Long duration, 6x potency.

Front 20

Enflurane

Back 20

Mx: gas anesthetic
Fx: isoflurane < blood:gas < halothane, potent MAC
S/E: ↓BP, ↓inotropy, n/c HR (unlike halothane/isoflurane). Rapid shallow breathing, strong hypoxia response depression, ↓PCO2 can cause convulsions (c/i epileptics)! Cerebral vasodilation, muscle/uterus relaxation, enhance curaroids, halothane-like renal fx.
Summary: Rapid, smooth, less arrhythmias+postop shivering+nausea+vomiting than halothane/methoxyflurane, more skeletal muscle relaxation than others, lots of circulatory/respiratory depression, seizures possible.

Front 21

Estrogen

Back 21

Mx: Hormone
Fx: ↓GnRH freq after long absence of menstrual cycle, ↓amplitude of FSH/LH except at midcycle. See progestin for more fx on reproductive tract.
Tx: OCP, replacement.
S/E: Replacement - CV: favorable lipids, no MI change, progestins reverse benefit. More thromboemboli, gallbladder dz. Endometrial CA↑ with pure estrogen, decrease w/progestins. Breast CA controversial, long use only. OCPs - no CV risk in nonsmokers, minimal thromboembolism, ↓endo+ova cancer, cysts, slight ↑liver ca/adenoma, slight ↑gallbladder probs, ↑hormone-binding globulins.

Front 22

Ethosuximide

Back 22

Mx: ↓Ca²⁺ T-channel conductance
Tx: Absence seizures! (are exacerbated by carbamezepine/phenytoin)
Kx: Fast absorb, HL 40hrs, 25% urine exc, 75% P450.
S/E: GI, head, restlessness, poor concentration.
D/I: Valproic acid ↑concentration (↓clearance).

Front 23

Fentanyl

Back 23

Mx: Opioid analgesic
Fx: Strong mu-opioid agonist. 100x as potent as morphine.
Kx: Short HL
Tx: Anesthetic adjunct (rapid fx/recovery) - IV, patch.
Else: See morphine.

Front 24

Finasteride

Back 24

Mx: 5a-reductase inhibitor (type II)
Fx: Blocks T→DHT in genitals
Tx: PO for BPH, androgenic alopecia
S/E: Rare impotence, endocrine fx

Front 25

Flumazenil

Back 25

Mx: Benzodiazepine antagonist.

Front 26

GABA

Back 26

Foo

Front 27

Gonadorelin

Back 27

Mx: Synthetic GnRH
Fx: Given pulsatile, 21 day regimen, SC pump.
Tx: Infertility - high percentage ovulated/conceived.
S/E: Only 7% multiple pregnancies, less ovarian hyperstim than others, but expensive.
Kx: HL 1-2min.

Front 28

Gonadotropin

Back 28

Mx: FSH/LH forms
Tx: Infertility - give FSH+LH forms (HP-axis not required!)
S/E: Multiple births (20-25%), severe ovarian enlargment (1% perotineum fluid), worse than clomiphene - try that 1st. Expense, injections, complex.

Front 29

Halothane

Back 29

Mx: gas anesthetic
Kx: Potent, high blood:gas (slow)
Tx: Maintenance of anesthesia, kids (less s/e), combined w/N2O for analgesia.
S/E: ↓BP, catecholamine sensitization (arrhythmias), shallow rapid breathing (not irritant), increase cerebral blood flow, some muscle relaxation, used prenatal but not in labor (inhibits contractions), ↓GFR/RPF reversible. HEPATIC NECROSIS/HEPATITIS, P450 INHIBITOR. MALIGNANT HYPERTHERMIA, tx w/DANTROLENE.

Front 30

Heroin

Back 30

Illegal, metab to morphine.

Front 31

Isoflurane

Back 31

Mx: gas anesthetic
Kx: Potent, rapid, mostly unmetabolized.
Tx: Most commonly used gas in US. Combined w/opioids/N2O to reduce conc.
S/E: ↓BP, but n/c CO. Lower tidal volume, normal RR rate. Resp irritant, pungent. No renal/hepatox. Potentates NMBs.
Benefits: No arrhythmias!

Front 32

Leuprolide

Back 32

Mx: GnRH super-agonist
Fx: Initial FSH/LH stim, long-term suppression ("chemical castration") - estrogen/testosterone production drops.
Kx: SC/implant, HL hours
Tx: Prostate cancer, precocious puberty, endometriosis, fibroids.

Front 33

Lidocaine

Back 33

Mx: Amide local anesthetic
Fx: Na⁺ blocker
Tx: Antiarrhythmic, anesthetic (injection, iontophoretic).
S/E: TINNITUS, drowsiness, nausea, dizziness, twitching, seizures, coma, respiratory depression.
Kx: Potency > procaine, onset > procaine, duration > procaine.

Front 34

Meperidine

Back 34

Mx: Opioid analgesic
Fx: Strong Mu-opioid agonist, plus antimuscarinic. Less potent but as effective as morphine.
C/I: Tachycardia
Else: See morphine.

Front 35

Methadone

Back 35

Mx: Opioid analgesic
Fx: Strong mu-agonist.
Kx: Longer lasting than morphine.
Tx: Chronic pain relief, detox.
Tol: Slower than morphine.
W/D: Milder than morphine.
Else: See morphine.

Front 36

Methamphetamine

Back 36

Mx: NE+DA releaser, reuptake inhibitor, MAO inhibitor
Fx: Central: ↑attentiveness, ↑motor task performance, anorexia, ↑locomotor/speech activity, ↑insomnia. Periph: NE-like, ↑BP, ↑arrhythmias/anigna, ↑urinary sphincter tone, mydriasis, ↑GI activity (cramps, diarrhea, vomiting).
Tx: None, can be PO/IV/smoked.
Tol: ↑↑↑psych dependence (DA reward mx). Rapid tolerance to most fx.
W/D: Exhaustion, depression, ↑appetite.
O/D: High dose: confusion, illusions, panic, suicidal/homicidal. V. high: psychosis (formication - tx chlorpromazine), vomiting, convulsions, coma.

Front 37

Methoxyflurane

Back 37

Mx: gas anesthetic
Kx: HIGHEST B:G, slowest!

Front 38

Mifepristone

Back 38

Mx: Antiprogesterone/antiglucocorticoid
Fx: Blocks progesterone receptors→decidual breakdown, detach embryo→↓hCG (more decidual breakdown), ↓progesterone = ↑prostaglandins, ↑uterine contractility, cervical softening.
Tx: Postcoital CP - 1 dose 100% fx within 72hr, pregnancy termination - 90% fx within 49 d w/misoprostol.

Front 39

Misoprostol

Back 39

Mx: Prostaglandin
Tx: Pregnancy termination w/mifepristone

Front 40

Morphine

Back 40

Mx: Opioid Anesthetic
Fx: Strong Mu-agonist (GPCR-Gi) - ↓Ca²⁺, ↑K⁺. ↓Release Glu, SubP, ACh, NE, 5HT. Actions: Analgesia, euphoria, ↓RR, sedation, cough suppression, miosis (important dx), emesis (w/o nausea), constipation, ↑GI tone, ↑CSF pressure 2⁰ to acidosis, ↑histamine, ↓hormones.
Kx: 4-6 hrs, active mets. Glucoronidated in liver, excreted in urine.
Tx: Analgesia
D/I: ↑depressant: phenothiazine, chlorpromazine, MAOis, TCAs. Enhance analgesia: Low dose amphetamine.
C/I: Full+partial agonist combo (precipitate w/d), head injuries, pregnancy (cross placenta), impaired pulm, impaired hepatic, addison/hypothyroid (↑response).
Tol: To euphoric, analgesic, sedative, ↓CNS fx. NOT TO MIOSIS/CONSTIPATION.
Eu: Immediate euphoria, relaxation, peace, ↑social, light sleep, ↓libido.
W/D: 6-10 hrs after last dose: Drug seeking, lacrimation, rhinorrhea, yawning, sweating. Then: restless sleep, mydriasis, tremor, piloerection, irritability. Then (for 7-10d): Insomnia, irritability, nausea, vomiting, diarrhea, chills, sweating, aches, movements, ↑RR, ↓weight, dehydration. Then (mos): ↓BP, ↓HR, ↓Temp, mydriasis. NOT LETHAL.
O/D: Death from respiratory depression.
Detox: Longer-lasting opioid (methadone) and taper. A2-agonist against symp s/e. Naltrexone.

Front 41

Muscarine

Back 41

Foo

Front 42

Naloxone

Back 42

Mx: Opioid antagonist
Fx: Mu-antagonist, N17 derivative of morphine.
Kx: Poor oral uptake, 1-2hr duration IV.
Tx: Opiate O/D. Note: because of short HL, severe O/D pt can "recover" then slip back after it wears off!

Front 43

Naltrexone

Back 43

Mx: Opioid antagonist
Fx: Mu-antagonist, N17 derivative of morphine.
Kx: Good PO uptake, HL 10hrs, 1 dose = 48 hr block of heroin fx.
Tx: Opiate O/D, chronic alcoholism.

Front 44

Neostigmine

Back 44

Mx: Reversible AChE inhibitor
Tx: Overcomes curaroids (shorter action of NMB) which act as competitive antagonists @ NIC receptor.

Front 45

Nicotine

Back 45

Mx: stimulant+depressant
Fx: Ganglion symp stim (↑HR, HTN), parasymp stim (↑GI), central stim (↑arousal, ↑rxn time, ↑learning), euphoria, nucleus accumbens ('reward mechanism').
W/D: Irritability, impatience, hostility, difficulty concentrating, depressed mood, restlessness, ↓HR, ↑weight gain, ↑appetite.
Treat with supplement.

Front 46

Nitrous oxide

Back 46

Mx: gas anesthetic
Kx: Very high MAC, very fast induction/recovery. Speeds up induction in combos.
Tx: Weak anesthetic alone, analgesic/sedative at < 80%, used as adjunct.
S/E: With halogens, ↑BP, ↑HR, ↑CO; opposite w/opioids. Diffusional hypoxia at high conc, use 100% O2 to compensate.

Front 47

NMDA

Back 47

Foo

Front 48

Norepinephrine

Back 48

Foo

Front 49

Norgestrel

Back 49

Mx: Progestin
Tx: Postcoital CP, 2 doses.

Front 50

Pancuronium

Back 50

Mx: Non-depolarizing NMB.
Fx: Competitive antagonist @ nicotinic receptor. Higher doses may block receptor. Sensitivity: face > eye > fingers > limbs/neck/trunk > intercostals/diaphragm. No CNS fx. Cardiac: low dose ↑HR, high dose ↓CO (histamine, ganglionic). ↓BP b/c histamine - pre-tx w/antihistamine.
ToxTx: Atropine (muscarinic antag), neostigmine.
Tx: Anesthesia adjunct, muscle relaxant, etc.
C/I: Asthma (histamine!), myasthenia gravis.
D/I: Local anesthetics may potentiate.
Specifics: Slight autonomic ganglia block, moderate cardiac muscarinic block (tachy!), no histamine release. Very long duration (kidney elim), 6x potency.

Front 51

Pentobarbital

Back 51

Kx: Short-acting, short-lasting barbiturate. Common illegal use.

Front 52

Phencyclidine

Back 52

Mx: Dissociative anesthetic, hallucigenic.
Fx: NMDA agonist, DA reuptake modulator(?)
S/E: Unresponsive/bizarre/violent behavior. Blank stare. High dose: analgesia, anesthesia, stupor/open eye coma, facial grimaces w/blank stare, inability to speak, ↑HR, ↑BP, psychosis (common).
O/D: ↑↑↑Temp, seizure, coma, rhabdomyolysis. Death!
O/DTx: Symptomatic. Suction, ventilation, cooling, diazepam (convulsions), hydralazine (vasodilator for ↑BP).
W/D: Not in humans. Usual in primates.

Route: Oral, nasal, injected, inhaled.

Front 53

Phenelzine

Back 53

Mx: Irriversible MAOi
D/I: Morphine (↑depression)
Careful: mixing w/amphetamines

Front 54

Phenobarbital

Back 54

Mx: GABA-A potentiator (and others...)
Fx: GABA-A prolonged opening, ↓Na⁺ conduction (AMPA activity), ↓AP generation, ↓d/c frequency, ↓Ca²⁺ conduction.
Tx: Febrile/recurrent seizures in kids, tonic/clonic seizures (if unresponsive to phenytoin/carbamezepine).
Kx: PO, P450 INDUCER.
S/E: Sedation, ocular, etc. Rebound seizures, cognitive depression when febrile seizure tx.

Front 55

Phenothiazine

Back 55

D/I: Morphine (↑depression)

Front 56

Phenytoin

Back 56

Mx: ↓Na⁺ influx, ↓Ca²⁺ influx.
Fx: Less excitation, less neurotransmitter release. Suppresses high frequency discharge/abnormal propagation, no ↓CNS, some drowsiness/lethargy - no hypnosis.
Tx: Partials, tonic-clonic, status epilepticus (2nd).
Kx: Slow PO (std), fast IV (status epilepticus). Rapid distribution, P450 metab (INDUCER), 24 hr HL (variable, can saturate).
S/E: GINGIVAL HYPERPLASIA, megaloblastic anemia (↓B12 absorb), ataxia, diplopia, nystagmus, hyperglycemia/glycosuria (↓insulin).
D/I: Lots! Increases metabolism of other antiseizure drugs, anticoags, OCPs, quinidine, methadone.

Front 57

Procaine

Back 57

Mx: Ester local anesthetic
Fx: Na⁺ blocker
Tx: Infiltration anesthetic/dx nerve block.
S/E: Allergy
Kx: Low potency, slow onset, short duration.
Tox: Low. Allergy to esters due to sulfonamide-competing metabolite.

Front 58

Progestin

Back 58

Mx: Feedback inhibition @ pituitary+hypothalamus
Fx: Decreases GnRH pulse frequency @ hypothalamus. Inhibit estrogen-induced pituitary FSH/LH spike @ midcycle. This inhibits ovulation (100% combo; 97% progestin-only). Other: vaginal luteal morphology w/scanty secretion, cervical morphology preg-like w/scanty viscous cellular mucus (major fx), uterine secretory phase rapid, thin+inactive chronic, increased egg transport in oviduct.
Tx: Contraception (repeat: no corpus lutea, no FSH/LH spike, no midcycle estrogen, no post-ov progesterone rise)
S/E: (Progestin-only) - unpredictable bleeding, mood changes, weight gain, ↓HDL, ↑LDL, ↓bone density.

Front 59

Raloxifene

Back 59

Mx: Selective estrogen receptor modulator (bone-specific)
Tx: Osteoporosis
S/E: Hot flashes, leg cramps, thromboembolism. May ↓breast CA.

Front 60

Serotonin

Back 60

Foo

Front 61

Succinylcholine

Back 61

Mx: Depolarizing NMB.
Fx: Initial depolarization, then insensitivity. Phase 1: depolarizing block (prolonged ACh response, twitching) then flaccid paralysis. Phase 2: insensitivity, even after depolarization (like non-depolarizing NMB).
Kx: Charged (not lipid soluble) - IV/IM, no PO. Very rapid onset (1min), short duration (5-10mins). Plasma esterase metab.
Tx: ECT, rapid intubation.
S/E: Arrhythmias (low dose slowing (tx w/atropine), high dose increase), muscle pain, malignant hyperthermia (combo w/halogen anes, tx w/dantrolene), caution w/myasthenia, ↑K⁺.
O/D: DO NOT USE NEOSTIGMINE, MAKES WORSE. Artificial resp if O/D.

Front 62

Tamoxifen

Back 62

Mx: Selective estrogen receptor modulator (no specificity to bone)
Tx: Don't use, endometrial fx.

Front 63

Testosterone

Back 63

Mx: Androgen
Kx: Inject every 2-3 wks, or PO (17a-form w/bad s/e) or patch (most on skin...transfer to females)
Tx: Hypogonadism, osteoporosis, aging, growth stim (prob w/epiphyses closing), gyne probs (s/e!), anabolic steroids, anemia (replaced by EPO)
S/E: Women - masculinization, children - epiphyseal closing, acne, men - suppress HP axis (infertility!), erythrocytosis (high dose), 17a-forms - hepatox, gynecomastia.

Front 64

Tetracaine

Back 64

Mx: Ester local anesthetic
Fx: Na⁺ blocker
Tx: Topical, replaced by bupivacaine.
Kx: Potency > procaine, duration > procaine.

Front 65

Tetrodotoxin

Back 65

Mx: Na⁺ blocker...probably distractor. Paralytic, blocks AP propagation.

Front 66

Thiopental

Back 66

Mx: Barbiturate, IV anesthetic
Tx: Standard for induction. Poor analgesic/relaxant, no antagonist. ↓cerebral pressure (UNLIKE gasses!)
S/E: High dose - myocardial depression. Depresses respiration.

Front 67

Tiagabine

Back 67

Mx: GABA reuptake inhibitor
Tx: Partial seizures
Kx: Fast absorb, P450 metab.
S/E: tiredness, dizziness, GI

Front 68

Tubocurarine

Back 68

Mx: Non-depolarizing NMB.
Fx: Competitive antagonist @ nicotinic receptor. Higher doses may block receptor. Sensitivity: face > eye > fingers > limbs/neck/trunk > intercostals/diaphragm. No CNS fx. Cardiac: low dose ↑HR, high dose ↓CO (histamine, ganglionic). ↓BP b/c histamine - pre-tx w/antihistamine.
ToxTx: Atropine (muscarinic antag), neostigmine.
Tx: Anesthesia adjunct, muscle relaxant, etc.
C/I: Asthma (histamine!), myasthenia gravis.
D/I: Local anesthetics may potentiate.
Specifics: Weak autonomic ganglia block, no cardiac muscarinic fx, moderate histamine release. Long duration. Renal elim/liver clearance.

Front 69

Ulipristal

Back 69

Mx: Progesterone partial agonist/antagonist
Tx: Postcoital CP, 1 dose within 5d

Front 70

Valproic acid

Back 70

Mx: Na⁺ inhibitor
Tx: Myoclonic seizures! Some tonic-clonic, 2nd for absence, some bipolar.
Kx: Fast absorb, peak ~2hr, HL 9-18hr, P450 metab.
S/E: GI, sedation (↑phenobarbital), tremor, hepatox, teratogenic (spina bifida).
D/I: Inhibits phenobarbital, phenytoin, carbamezepine, ethosuximide metab.

Front 71

Local anesthetic mechanism

Back 71

Na⁺ blocker.
Progression: ↑excitation threshold→↓action potential rise rate→↓impulse conduction rate→↓prob AP propagation→nerve conduction fail.
Fx: Stronger in active neurons. Stabilizes inactive channel conformation.
Fx progression: Lose pain→cold→warm→touch→deep pressure.
Fx (pH): Anesthetic is weak base. pH 7.2: block channel. pH 9.6: no block. REPEATED INJECTION LOSES EFFECTIVENESS (local acidosis of hydrochloride salts).
Epi: Give epi w/drug to vasoconstrict, concentrating drug.
Esters: allergy, fast metab, cholinesterase deficiency monitor.
Amides: slow metab, liver fxn monitor.

Front 72

Local anesthetic duration

Back 72

Procaine < Lidocaine/Cocaine < Tetracaine/Bupivacaine < Dubicaine