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139 Cards in this Set

  • Front
  • Back
Inhaled Agents
General Anesthetics
Inhaled Agents

Mech: nebulous, likely ↑GABAA activity
SE: respiratory depression, ↓BP, hypothermia, nausea, ↑ICP; Emergence: ↑BP, tachy
Halothane
General Anesthetics
Inhaled Agents

MAC 0.75; Blood/Gas 2.54; slow induction/awakening; SE: ↑catecholamine sensitivity, myocardial depression, hepatic necrosis, malignant hyperthermia
Isoflurane
General Anesthetics
Inhaled Agents

MAC 1.17; B/G 1.46; common, $$, faster, useful in neurosurgery (↓ cerebral O2 consumption), low toxicity, pungent odor (no induction); SE: ↑HR
Sevoflurane
General Anesthetics
Inhaled Agents

MAC 1.80; B/G 0.69; rapid induction/awakening, least irritating, safest for CV disease (least ↓BP)
Desflurane
General Anesthetics
Inhaled Agents

MAC 6.60; B/G 0.42; most rapid, low toxicity, irritating (no induction); SE: ↑HR
Nitrous Oxide
General Anesthetics
Inhaled Agents

MAC 105, B/G 0.46; rapid, adjuvant to increase rate of induction w/ other agents, analgesia, diffusion hypoxia, attenuates hypotension; SE: nausea; Toxicity: megaloblastic anemia, peripheral neuropathy, abuse
IV Agents
General Anesthetics
IV Agents

Mech: ↑GABAA activity
Thiopental
General Anesthetics
IV Agents

barbiturate, not really used anymore, CI: porphyria
Midazolam (Versed)
General Anesthetics
IV Agents

ultrashort acting, sedation, ↓anxiety, amnesia, IV; reversed w/ Flumazenil
Propofol
General Anesthetics
IV Agents

DOC anesthetic, rapid on/off, ↓cerebral blood flow→ ↓ICP SE: respiratory depression, ↓BP w/ no ↑HR, anaphylactic rxn (eggs, albumin)
Etomidate
General Anesthetics
IV Agents

no BP effect; SE: nausea
Ketamine
General Anesthetics
IV Agents

NMDA antagonist, dissociative effect, analgesia, little resp. dep. or nausea, date rape drug; SE: emergence delirium in adults
Fentany
General Anesthetics
Opioid Analgesics

IV opioid for analgesia, rapid, lollipops, reversed w/ Naloxone (Narcan)
Local Anesthetics
Local Anesthetics

Mech: block Na channels, higher affinity activated channels, base form crosses membrane; Inflammation→ ↓body pH →↑ionized drug→ ↓effect
[BH+] / [B] = 10(pKa – pH)
Carbonation - ↓ intracellular pH→ ↑ intracellular drug[ ]; Vasoconstrictors (Epi) ↓drug diffusion away from site
Toxicity: CNS – tongue numb/metallic taste, aud/vis disturbance, twitching, convulsions;
CV – arrhythmias; PABA (esters) allergy
Esters
Local Anesthetics


Esters – one “i”, metabolized in blood by pseudocholinesterase
Procaine (Novocain)
Local Anesthetics
Esters

short axn, PABA inhibits sulfonamides
Tetracaine (Pontocaine)
Local Anesthetics
Esters

slower, longer, spinal anesthesia, w/ 10% dextrose to ↑specific gravity in CSF
Benzocaine
Local Anesthetics
Esters

topical for sunburn (tooth – Anbesol), OTC
Cocaine
Local Anesthetics
Esters

short axn, topical, blocks NE reuptake, vaso-c, tachy
Amides
Local Anesthetics
Amides

two “i’s”, metabolized in liver
Lidocaine (Xylocaine)
Local Anesthetics
Amides

rapid onset, intermediate duration, infiltration & epidural,
Bupivacaine (Marcaine)
Local Anesthetics
Amides

long duration, infiltration & epidural; SE: cardiotoxicity
Ropivacaine (Naropin)
Local Anesthetics
Amides

long duration, S-isomer (Bup is racemic); ↓lipid soluble, ↓cardiotoxic
Mepivacaine (Carbocaine)
Local Anesthetics
Amides

int duration
Prilocaine (Citanest)
Local Anesthetics
Amides

SE: methemoglobinemia; CI: CV or respiratory disease
Anticonvulsants
Anticonvulsants

Seizures – Partial: Simple – jerking, ~20 sec, preservation of consciousness
Complex – impaired consciousness <2 min
Generalized: Tonic-Clonic (Grand Mal) – loss of consciousness, muscle contractions
Absence (Petit Mal) – staring, ~30 sec
Myoclonic – brief muscle contraction
Possible due to ↓GABA or ↑Glutamate (NMDA) activity
CI: pregnancy
Phenytoin (Dilantin)
Anticonvulsants

prolongs Na channel inactivation; Tx: partial & tonic-clonic seizures; Induces P450, ↑ [warfarin], ↑oral contraceptive metabolism, dose dependent elimination; SE: gingival hyperplasia, hirsutism
Carbamazepine
Anticonvulsants

blocks Na channels; Tx: partial(DOC) & tonic-clonic seizures, trigeminal neuralgia, bipolar disorder; Drug intraxns, induces P450, SE: blood dyscrasias, GI upset;
Phenobarbital
Anticonvulsants

– prolongs Cl- opening at GABA; Barbiturate; Tx: partial & tonic-clonic
Gabapentin (Neurontin)
Anticonvulsants

GABA analog but nebulous mech; Tx: adjunct for partial & tonic- clonic seizures, neuropathic pain, bipolar disorder; kidney excretion
Pregabalin (Lyrica)
Anticonvulsants

tx: neuropathic pain, fibromyalgia
Topiramate
Anticonvulsants

blocks Na, ↑GABA, ↓glutamate
Ethosuximide
Anticonvulsants

↓Ca current in thalamus; Tx: absence seizures(DOC); SE: GI pain
Valproic Acid
Anticonvulsants

↓repetitive firing; Tx: absence + tonic-clonic(DOC), myoclonic, bipolar, migraine; SE: hepatotoxicity; Many drug intraxns
Clonazepam (Klonopin)
Anticonvulsants

Tx: absence seizures
Diazepam (Valium)
Anticonvulsants

Tx: status epilepticus(DOC
Stevens-Johnson Syndrome
Hypersensitivity autoimmune (immune complex) reaction; can happen w/ anticonvulsants; Epidermis separates from dermis; Tx: discontinue drug
Erythema multiforme, arthritis, nephritis, CNS abnormalities, myocarditis
Opioid Analgesics (Narcotics)
Also inhibit GABA →↓inhibition of inhibitory pain fibers (3 inhibitions) →↓pain
Opioid Effects – analgesia (sensory & affective), sedation, euphoria/dysphoria, antitussive, respiratory depression, ↑ICP, miosis, constipation, antidiuresis
Tolerance – High: analgesia, euphoria, sedation; Minimal: miosis, constipation
Intraxns – MAOI’s: hyperpyrexic coma; Tx: pain, cough, diarrhea, anesthesia, pulmonary edema
CI: head injuries (↑ICP); pregnancy; pts w/ impaired pulmonary, renal, or hepatic function
OD: CNS depression, ↓ respiration, miosis →mydriasis (hypoxic, near death)
Withdrawal: dysphoria, diarrhea, rhinorrhea, insomnia, anxiety, vomiting, hostility, more prone to certain infections
Opiate receptors
– Gi, close presynaptic Ca channels→ ↓transmitter release (sub P, Ach, NE, 5HT, glutamate); open postsynaptic K channels (μ)→ hyperpolarize
Mu (μ) – euphoria, analgesia, sedation, miosis, ↓GI motility
Kappa (κ) – dysphoria, analgesia, miosis
Delta (δ) – dysphoria, hallucinations, mydriasis
Morphine
Opioid Analgesics (Narcotics)
Strong Agonists

binds μ,κ,δ; ext 1st pass (oral); t1/2= 2hrs; Liver metabolism 1o; Conjugated to 3- glucuronide →antagonizes morphine & 6- which is more potent analgesic; Schedule II; Causes histamine release→ peripheral vaso-D, ↓BP
Hydromorphone (Dilaudid)
Opioid Analgesics (Narcotics)
Strong Agonists

morphine derivative; stronger, faster
Hydrocodone
Opioid Analgesics (Narcotics)
Strong Agonists

oral; Metabolism: Cyp2D6; inhibitors will ↓analgesia (quinidine, SSRI’s)
Vicodin, Lortab, Lorcet
Opioid Analgesics (Narcotics)
Strong Agonists

hydrocodone/acetaminophen
Oxycodone (OxyContin)
Opioid Analgesics (Narcotics)
Strong Agonists

oral; Tx: pain, restless leg, Tourette’s; Liver met – Cyp2D6
Percocet
Opioid Analgesics (Narcotics)
Strong Agonists

oxycodone/acetaminophen
Meperidine (Demerol)
Opioid Analgesics (Narcotics)
Strong Agonists

oral/parenteral; short acting; Dilates pupils; No antitussive; antimuscarinic; blocks 5HT reuptake, addictive; metabolite: normeperidine →anxiety, seizures, kidney exc, not reversed by naloxone; MPTP →parkinson’s
Methadone
Opioid Analgesics (Narcotics)
Strong Agonists

oral/rectal; longer axn; milder withdrawal; Tx: pain, heroin addicts, w/drawal
Fentanyl
Opioid Analgesics (Narcotics)
Strong Agonists

100x morphine, shorter axn; Met: Cyp3A4 (ind/inh will cause intraxns);
Tx: chronic pain, induction, anesthesia (maintains cardiac stability in surgery, attenuates hemodynamic response→ less ↓BP)
Alfentanil
Opioid Analgesics (Narcotics)
Strong Agonists

10x morphine; shorter axn than fentanyl; $$; Met: Cyp3A4
Sufentanil
Opioid Analgesics (Narcotics)
Strong Agonists

1000x morphine
Heroin
Opioid Analgesics (Narcotics)
Strong Agonists

passes BBB; 10x morphine; metabolized to morphine
Codeine
Opioid Analgesics (Narcotics)
Moderate Agonists

must be metabolized by Cyp2D6 →morphine (inh by quinidine, SSRI’s); Tx: mild pain, antitussive; low addiction potential
Tylenol 3
Opioid Analgesics (Narcotics)
Moderate Agonists

codeine/acetaminophen
Propoxyphene
Opioid Analgesics (Narcotics)
Moderate Agonists

like codeine, more toxic; high dose →seizure, psychosis
Darvocet
Opioid Analgesics (Narcotics)
Moderate Agonists

propoxyphene/acetaminophen
Pentazocine
Opioid Analgesics (Narcotics)
Mixed Agonists/Antagonists

agonist on κ, partial agonist on μ; less effective than morphine, more hallucinations
Buprenorphine
Opioid Analgesics (Narcotics)
Mixed Agonists/Antagonists

partial agonist on μ&κ; Tx: heroin addiction; IV, sublingual, intranasal; sublingual combined w/ naloxone (not absorbed sub-L) to prevent IV abuse
Tramadol
Opioid Analgesics (Narcotics)
Mixed Agonists/Antagonists

weak μ agonist; Inh reuptake of 5HT & NE; mild SE’s; Tx: moderate pain
Dextromethorphan (Robitussin)
Opioid Analgesics (Narcotics)
Antitussives

no analgesic or addictive properties; CI: MAOI’s
Codeine
Opioid Analgesics (Narcotics)
Antitussives
Naloxone (Narcan)
Opioid Analgesics (Narcotics)
Antagonists

IV; short axn; can precipitate withdrawal symptoms
Naltrexone (ReVia)
Opioid Analgesics (Narcotics)
Antagonists

Oral; long axn; used to prevent the opiate high
Nalmefene (Revex)
Opioid Analgesics (Narcotics)
Antagonists

like naloxone but longer axn
Autocoids
Autocoids

Phospholipase A2 – takes membrane phospholipids → Arachidonic Acid
COX-1
Autocoids

PG’s, TX’s; constituitive; protects gastric mucosa, +platelet aggregation, vaso-C
COX-2
Autocoids

PG’s, TX’s; inducible; +inflammation, inh platelet agg; vaso-D
Lipoxygenase
Autocoids

Leukotrienes
PGI
Autocoids

vaso-D, broncho-D, ↑GFR; Tx: pulm HTN
PGE
Autocoids

vaso-D, broncho-D, ↑GFR, uterine contraction; Tx: abortion, induce labor, penile injection for ED, maintain patent DA, GI protection (Misoprostol)
PGF
Autocoids

broncho-C, uterine contraction, Tx: glaucoma [Latanoprost – (Xalatan)]
TXA
Autocoids

vaso-C, broncho-C
NSAID’s
-Acetylsalicylic Acid (Aspirin) – irreversibly inh COX-1 & 2; anti-inflammatory, analgesic, antipyretic, inh platelets; kidney exc; initial ↑respiration, then ↓; low dose →↓uric acid excretion, high dose →↑uric acid exc; induces asthma; ↑GI acid, ↓PG’s →ulcers; Long term→ kidney damage; Reye’s Syndrome – cerebral edema in kids w/ viral inf
Diflunisal, Salsalate
NSAID’s
Salicylates

Tx: RA, OA, pain
Celecoxib (Celebrex)
NSAID’s
COX-2 Inhibitors

COX-2 inh (cox-2:1 inh 7:1); fewer GI SE’s
Rofecoxib (Vioxx)
NSAID’s
COX-2 Inhibitors

COX-2 inh (cox-2:1 inh 70:1); Blood clotting CV events, w/drawn
Indomethacin
NSAID’s
Nonspecific COX Inhibitors

– inh Phospholipase A2, inh PMN migration; potent; most SE’s; Tx: close PDA
Diclofenac
NSAID’s
Nonspecific COX Inhibitors

inh COX
Arthrotec
NSAID’s
Nonspecific COX Inhibitors

diclofenac/misoprostol
Ketorolac
NSAID’s
Nonspecific COX Inhibitors

inh COX; potent; oral/IV/IM Tx: post-op pain, use max 5 days (SE’s)
Ibuprofen
NSAID’s
Nonspecific COX Inhibitors

inh COX; analgesia, antipyretic, anti-inf; low SE’s; ↓ASA effect; Tx: OA, RA
Naproxen (Naprosyn, Aleve)
NSAID’s
Nonspecific COX Inhibitors

like ibuprofen; long t1/2; CI: pregnancy
Piroxicam
NSAID’s
Nonspecific COX Inhibitors

↓ROS, inh PMN migration; long t1/2, many SE’s
Nabumetone
NSAID’s
Nonspecific COX Inhibitors

long t1/2, few SE’s
Etodolac
NSAID’s
Nonspecific COX Inhibitors
Excedrin
NSAID’s
Nonspecific COX Inhibitors

acetaminophen/aspirin/caffeine
Acetaminophen/Paracetamol (Tylenol)
NSAID’s
Other

nebulous mech; antipyretic, analgesic, no anti-inf; safe at therapeutic doses; Toxicity: hepatotoxicity (10-15g), hepatic necrosis (25g), toxic metabolite exceeds GSH levels; Toxicity Tx: n-acetylcysteine (Mucomyst)
DMARD’s
DMARD’s take weeks to months for full effect
Methotrexate
DMARD’s

inh dihydrofolate reductase (DHFR)→ ↓DNA synthesis & maybe ↓T-cell activation; CI: pregnancy, liver disease
Aurothioglucose
DMARD’s

oral/parenteral; gold salts; inh phagocytosis, ↓PG’s, ↓proteolytic enzymes
Penicillamine
DMARD’s

oral; chelating agent, ↓T-cell activity, ↓IgM Rheumatoid Factor, inh collagen synthesis; adverse rxns
Hydroxychloroquine (Plaquenil)
DMARD’s

oral; antihistamine, anti-Ach, antiprotease, ↓PG’s, ↓chemotaxis; SE: hemolysis in G6PD def
Sulfasalazine
DMARD’s

oral; maybe inh COX & LO; well tolerated; Tx: RA, IBD; SE: GI upset
Infliximab (Remicade)
DMARD’s

IV; chimeric IgG against TNF-α; Tx RA w/ methotrexate
Rituximab
DMARD’s

IV; chimeric IgG against CD20 (B-cell); Tx: RA, non-Hodgkin Lymphoma
Adalimumab (Humira)
DMARD’s

SC; human IgG against TNF-α; Monotherapy for RA; SE: rash, flu- like symptoms
Etanercept (Enbrel)
DMARD’s

IV/SC; TNF-α receptor fusion protein, binds and inactivates TNF
Abatacept
DMARD’s

IV; human recombinant fusion protein, blocks T-cell activation
Leflunomide
DMARD’s

oral; inh DHODH→ ↓pyrimidine synthesis; inh COX-2
Mycophenolate Mofetil (MMF)
DMARD’s

oral/IV; prodrug, inh IMPDH→ ↓lymph purine synthesis
Anakinra
DMARD’s

– SC; IL-1 Receptor antagonist (IL-1Ra); monotherapy or w/ other DMARD
Drugs for The Gout
Drugs for The Gout

Drugs CI in The Gout: Thiazide & Loop diuretics, Triamterene, Aspirin, Etoh, more
Colchicine
Drugs for The Gout
Drugs for Acute Attacks

oral; binds tubulin→ inh microtubules→ inh PMN activity, ↓inf; no analgesia; SE: diarrhea; used prophylactically w/ uricosuric agents
Indomethacin, Naproxen, Celecoxib
Drugs for The Gout
Drugs for Acute Attacks
NSAID's

CI: aspirin b/c ↓ uric acid excretion
Drugs for Hyperuricemia
Uricosuric Agents
Drugs for The Gout
Drugs for Hyperuricemia

Block active reabsorption of uric acid in proximal tubule
SE: kidney stones (drink lots of water), ↓excretion of other acidic compounds
May trigger gouty attack (prophylax w/ colchicine); Not used in acute attacks
Probenecid
Drugs for The Gout
Uricosuric Agents
Sulfinpyrazone
Drugs for The Gout
Uricosuric Agents

inh platelet agg, inh warfarin metabolism
Allopurinol
Drugs for The Gout
Xanthine Oxidase Inhibitors

inh XO: blocks purines→hypoxanthine→xanthine→uric acid; may trigger gouty attack; inh metabolism of warfarin & probenecid
Rasburicase
Drugs for The Gout
Other

recombinant urate oxidase (not endogenous in humans) from Aspergillus; uric acid→ allantoin (readily excreted); Anaphylaxis on 2nd admin possible
Migraine Drugs
Migraine Drugs

Migraine – throbbing, 2-72 hrs, visual auras, photosensitivity, nausea
First phase – intracranial vaso-C, ischemic changes, prodromic visual aura
Second phase – extracranial vaso-D, vasoactive material release→ pain, inf
Cluster – excruciating pain, around eyes, during sleep 15-90 min
Tension – stress onset, dull, persistent, tightening, 30 min – 7 days
Sumatriptan (Imitrex)
Migraine Drugs
Symptomatic Treatment
5HT Agonists

5HT1D&1B agonist →vaso-C intracranial; oral/SC; SE: vasospasm, stroke, intracranial bleeding, peripheral ischemia; CI: PAD, CAD, cerebrovascular disease; Tx: acute migraine
Naratriptan, Rizatriptan, Eletriptan, etc.
Migraine Drugs
Symptomatic Treatment
5HT Agonists
Aspirin, Acetaminophen, Codeine, etc.
Migraine Drugs
Symptomatic Treatment
Analgesics
Naproxen, Ibuprofen, etc
Migraine Drugs
Symptomatic Treatment
NSAID’s
Ergot Alkaloid
Migraine Drugs
Prophylaxis

ergot is a fungus, grows on rye ; wet season→ Ergotism (St. Anthony’s Fire): vaso-C (burning), gangrene, hallucinations
Ergotamine
Migraine Drugs
Prophylaxis

partial agonist 5HT & α receptors; Tx: migraine during prodrome SE: ergotism
Methysergide (Sansert)
Migraine Drugs
Prophylaxis

partial agonist on 5HT, weak vaso-C; Tx: migraine prophylaxis; SE: retroperitoneal fibrosis
ß-Blockers
Migraine Drugs
Prophylaxis

Propanolol
Calcium Channel Blockers
Migraine Drugs
Prophylaxis

Verapamil
Antidepressants
Migraine Drugs
Prophylaxis

Amitriptyline, Lithium Carbonate, Valproic Acid, Topiramate
Female Hormones
Migraine Drugs
Prophylaxis

Estradiol
Drugs of Abuse
-Cocaine
-Methamphetamine
-Nicotine
-Caffeine
-Alcohol
-Benzodiazepines
-Opioids
-Marijuana
-LSD
-Mescaline
-MDMA (Ecstasy)
-Phencyclidine (PCP, Angel Dust)
-Ketamine (Special K)
-Inhaled
Drugs Affecting Coagulation
Intrinsic – XII, XI, IX, VIII; PTT time
Extrinsic – TF, VII; PT time, INR
Common – X, V, II, I
Collagen – vWF – GP1b
GPIIb/IIIa - Fibrinogen
Platelet activation - ADP, TXA2, 5HT
Anticoagulation – TFPI, Thrombomodulin, ATIII
Fibrinolysis – Plasminogen→ Plasmin, Protein C, t-PA, urokinase, streptokinase
Heparin sodium
Drugs Affecting Coagulation
Anticoagulants

IV; accelerates ATIII axn; ↑PTT time; axn prolonged in renal/hepatic dys
Enoxaparin (Lovenox)
Drugs Affecting Coagulation
Anticoagulants

– LMWH; SC; SE: HIT; CI: intracranial hemorrhage, renal/hepatic disease; Useful in pregnancy, doesn’t cross placenta
Lepirudin
Drugs Affecting Coagulation
Anticoagulants

direct inh thrombin; leeches; Renal exc; difficult to reverse; Tx: HIT
Argatroban
Drugs Affecting Coagulation
Anticoagulants

direct inh thrombin; Liver met; difficult to reverse; Tx: HIT
Warfarin (Coumadin)
Drugs Affecting Coagulation
Anticoagulants

Vit K analog, ↓II, VII, IX, X; sweet clover, rat poison; monitor w/ PT/INR; Initial ↑clotting (rapid ↓protein C); Effect takes 12-16 hrs to develop; 98% plasma protein bound; oral contraceptives ↓effect; Cimetidine ↑effect
Reversal – Vit K, FFP, Factor IX
Anticoagulant Reversal Agents
Protamine sulfate
Drugs Affecting Coagulation
Anticoagulant Reversal Agents

heparin antagonist; In absence of heparin, anticoagulant effect
Vitamin K1
Drugs Affecting Coagulation
Anticoagulant Reversal Agents

warfarin reversal
Tissue plasminogen activator (t-PA)
Drugs Affecting Coagulation
Fibrinolytic Agents

activates plasminogen→ plasmin; $$
Streptokinase
Drugs Affecting Coagulation
Fibrinolytic Agents

fibrinolytic; may cause AB formation→ allergic response, ↓efficacy
Urokinase
Drugs Affecting Coagulation
Fibrinolytic Agents

activates plasminogen→ plasmin
Anistreplase
Drugs Affecting Coagulation
Fibrinolytic Agents

plasminogen/streptokinase
Aminocaproic acid
Drugs Affecting Coagulation
Antifibrinolytic Agents

inh plasminogen activation; Tx: bleeding disorders, reverse fibrinolytic agents
Aspirin
Drugs Affecting Coagulation
Antiplatelet Agents (Antithrombotics)

↓platelet agg, irreversible for life of platelet (7-10 days)
Clopidogrel (Plavix)
Drugs Affecting Coagulation
Antiplatelet Agents (Antithrombotics)

oral; inh ADP in platelet; less GI SE’s than aspirin
Abciximab (ReoPro)
Drugs Affecting Coagulation
Antiplatelet Agents (Antithrombotics)

IV; inh GPIIb/IIIa; $$
Eptifibatide (Integrilin)
Drugs Affecting Coagulation
Antiplatelet Agents (Antithrombotics)

IV; inh GPIIb/IIIa; rattle snake venom derived
Tirofiban (Aggrastat)
Drugs Affecting Coagulation
Antiplatelet Agents (Antithrombotics)

IV; inh GPIIb/IIIa