Professional Documents
Culture Documents
Nicotine Nicotinic
Acetylcholine Augmenters
Propantheline Synthetic
Tubocurarine Given IV or IM
Unknown; Decreases Ca
Dantrolene Malignant hyperthermia Hepatotoxicity
release from SR
Blocks Ach vesicle Prevent sweating,
Botulinum toxin
release (for months) cosmetic
Black Widow Spider Massive release of Ach
Venom from vesicles
Direct: a
Metaraminol Hypotensive states No CNS-too polar
Indirect: rel. of Norepi
Alpha-Adrenergic Antagonists
Doxazosin
Prazosin
Beta-Adrenergic Antagonists
Bronchoconstriction,
Propranolol HTN, glaucoma, arrhythmias at
migraine, CV, thyroid, withdrawl
Non-selective beta stage fright
Nadolol longer duration
blocker
Local Anesthetics
Short-acting, Ester
Procaine
(PABA metabolites)
Anesthetic… blocks C- CV, CNS depression,
Lidocaine Blockade of Na+ channel Intermediate-acting
fibers, then Adelta- Antiarrhythmic
in membrane… prevents
fibers, then Aalpha
Bupivacaine depolarization Long-acting
motor fibers
Surgery, Recreational Minor CV, resp and SM Gas, rapid onset and
Nitrous Oxide
(Whip-its) effects, CNS toxicity recovery (low lipophilic)
Blunts resp, CV, uterus, No analgesic effect,
Halothane
Malignant hyperthermia reactve metabltes->Hep
Surgery
Ion channels, signal Greater Resp. Used a lot, not good
Isoflurane
transduction depression, bad odor with longer procedures
Analgesics, not much Most potent of gas
Methoxyflurane Labor and delivery
uteran; Nephrotoxicity agents
CNS Depression
Thiopental GABA receptors Resp and CV toxicity Induction Agent
(anesthetic)
Midazolam, Valium Potentiation of GABA Conscious sedation with Countered with
(Benzodiazepines) (inhibitory effects) amnesia Flumazenil
Induction (replaced
Propofol Decreased TPR
Thiopental)
Vomiting, Nausea, pain
Ethomidate Hypnotic No analgesic effects
on injection
Replaced morphine and
Fentanyl (Opiods) Analgesia w/ amnesia Less CV effects
meperidine
Catatonia without CV or Similar to PCP: weird
Ketamine NMDA antagonist Dissociative anesthetic
Resp depression dreams/visions, inc ICP
Benztropine
Reduce excitation of Muscarinic blockade:
Anticholinergic agents
GABA neurons Can't see,spit,pee,shit
Trihexyphenidyl
Reserpine
Antipsychotics Huntington's Chorea Do not work very well
Tetrabenazine (Dopamine Tardive Dyskinesia
antagonists/depletors)
Haloperidol Tics (Tourette's)
Also antiemetic,
Chlorpromazine First antipsychotic drug
antihiccup
Arrhythmias w/
High sedation, alpha-
Thioridazine overdose Pigmentary
blockade, Low EPS
retinopathy
Depot preparation for
Fluphenazine
compliance probs
Classical antipsychotics
- Reduce dopamine
action
Perphenazine
Classical antipsychotics
Prochlorperazine - Reduce dopamine
action
Thioxanthines
Thiothixene
Butyrophenones
Possible birth defects, Also used for pain control, diabetic neuropathies,
Antiepileptic Drugs
OC interactions and withdrawl symptoms control
Like Phenytoin; + DOC Drowsiness, vertigo,
Carbamazepine NOT used for Absence
for Trigeminal Neuralgia ataxia
Block Na channels in
+ (petit mal) seizures;
Tonic-clonic (GM), Gingival hyperplasia, zero-order at [high]
Phenytoin (1o) brain; reduce neuron
Psychomotor, and Focal nystagms,atxia,hirsutsm
firing
Block Na+ channels in
brain; reduce neuron
firing
More hydrophilic IM/IV;
Fosphenytoin
In ER for FAST action
Valproic acid (2o) Prolongs GABA, Blocks Anticonvulsant and Liver failure in kids
(Valproate) Na+ and T-type Ca2+ mood-stabilizer (with overdose)
GM, Psychomotor, and Sedation or Least toxic; --> Children
Phenobarbital
Focal; also (EtOH w/x) hyperactivity to avoid gum growth
Metabolized to Allows for greater activity with less blood levels of
Primidone Myoclonic in children
Phenobarbitol and PEMA Phenobarbital, therefore less sedation
Blocks T-type Ca2+ Absence (petit mal) Extended depression
Ethosuximide (1o) Contra in tonic-clonics
channels ONLY -- usually children (GI, drowsiness, lazy)
Useful in all, esp. Drowsiness, ataxia, Potential to exacerbate
Clonazepam Stimulates GABA
myoclonic and akinetic aggressiveness seizures; yes Tolerance
Levetiracetam Partial sz
Opioid Antagonists
Opioid toxicity (Resp. Can try in ER with Talwin-NX (no
Naloxone
Pure antagonist (mainly depression, coma) comatose pt. absorption orally)
at Mu receptors) Longer onset, T1/2,
Naltrexone Opioid, EtOH addiction
duration of action
Miscellaneous
Daytime anxiety,
Triazolam For starting sleep Shorter-acting
morning insomnia
Hasten recovery, Also antagonizes
Flumazenil BZ receptor antagonist
overdose zolpidem and zaleplon
Also used for Panic disorder, Enuresis, Chronic No CNS stimulation for
Drugs for Depression
pain, Eating disorders, Attention Deficit disorder normal patients
MAOa = NE, 5-HT
Monoamine Oxidase Inhibitors Nasty drugs
MAOb = DA
Tricyclic Antidepressants
Higher incidence of
Amitriptyline Very low TI; OD can be
anticholinergic
fatal (treat symptoms);
potentiate
amphetamines (block
Block reuptake of 5-HT reuptake); counter
and NE Guanethidine and
Clonidine (HTN), and L-
Very low TI; OD can be
fatal (treat symptoms);
Clomipramine potentiate
Similar to antipsychotics amphetamines (block
Block reuptake of 5-HT (block alpha, histamine, reuptake); counter
Desipramine muscarinic receptors)
and NE Guanethidine and
BUT don't block DA Clonidine (HTN), and L-
Imipramine receptors dopa due to delayed
(so you see arrythmias, gastric emptying
constipation, seizures) (antimuscarinic)
Nortriptyline
Requires downregulation
High TI (death only with
Selective Serotonin Reuptake Inhibitors of autoreceptor 4
combos)
activity
Long T1/2 of metabolite
Fluoxetine (Prozac)
CNS stimulation, sexual (least w/x sx)
dysfunction; inhibition
Fluvoxamine of P-450 (esp.
Block reuptake of 5-HT
fluoxetine, paroxetine);
selectively
Paroxetine Serotonin syndrome
(esp. w/
MAOIs/meperidine)
Sertraline (Zoloft)
Other Antidepressants
Bupropion
Inhibits presynaptic
Mirtazapine
alpha 2 receptors
Inhibits reuptake of NE
Venlafaxine
and 5-HT
Nefazodone
Hypothalamic-Pituitary Drugs
GnRH receptor
Abarelix Prostate cancer
antagonist
Triamcinolone
Gonadal Drugs/Hormones
Selective estrogen
Tamoxifen Binds to receptor
receptor modulator
Breast cancer
Anastrozole
Aromatase inhibitors
Letrozole
Pancreatic Drugs/Hormones
Sulfonylureas (1o)
Act on K+ channel to Disulfiram-like rxn
(Glyburide)
make B cell release Type II diabetes Short-acting; target
insulin Hypoglycemia, Drug
Repaglinide post-prandial glucose
interactions (EtOH)
spikes
Biguanides (1o) Decrease gluconeo- Mainly Type II (if no Glucose enters SM and
(Metformin) genesis, increase usage hepatic/renal disease) adipocytes
Thiazolidinediones Reduces peripheral P450 inducer, edema,
Activated PPAR-gamma
(TZD) (Pioglitazone) insulin resistance volume expansion
Glucosidase inhibitor -
Acarbose Flatulence
reduces uptake frm gut
Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous
Drugs of Abuse
Caffeine
Ephedrine
Methylphenidate
Phentermine
Sibutramine
Ketamine
"Breaking phenomenon" Some allergies to sulfur Passive Na exchange Increase LDL, TGs, and
Thiazide Diuretics
with all Na excretors in structure distally can --> K loss total cholesterol
Furosemide
Hypovolemia,
1o: Inhibit Na,K,Cl
hypokalemia,
Ethacrynic acid symporter in thick Edema, acute renal
hypocalcemia,
ascending limb failure, hypercalcemia, Also INCREASE Ca2+ in
hyperuricemia,
2o: inhibit NaCl chemical intoxication urine
Bumetanide ototoxicity (esp. E.
symporter in distal (increases excretion)
acid), impaired platelet
tubule
aggregation
Torsemide
Xanthines
Diuretics
Hydrochlorothiazide
See above
Furosemide
Beta-adrenergic Antagonists
Propranolol
Reduce CO, and plasma
Metoprolol renin activity; also Cardiosensitive (Beta1)
Bronchoconstriction
inhibit presynaptic beta HTN
(except with metoprolol)
Nadolol receptors, CNS effects,
PNS effects
Pindolol
Alpha-adrenergic Antagonists
Centrally-acting Drugs
Diltiazem
HTN, Arrythmias (slow
Reflex tachycardia may
conduction through AV
Nifedipine Calcium channel blocker worsen heart condition,
node, DECREASE
effects on AV conduction
contractility) Avoid in those with
Verapamil
conduction disturbances
Nitroglycerin (IV)
Activation of guanylyl Excessive dilation -->
cyclase --> inc. cGMP Hypotension
Nitroprusside Releases nitric oxide
Activation of ATP-
Minoxidil
sensitive K channels
Ca channel blocker,
Hydralazine Preeclampsia
inhibits enzymes ->ROS
arteriolar dilation, also
Fenoldopam Dopamine (D1) agonist Hypokalemia
afferent AND efferent
Drugs that Alter Hemostasis
Antiplatelet Drugs
Warfarin Sodium Prevents carboxylation of Vitamin K - prevents Bleeding, allergy;Contra Oral; genetic variations
(coumarin) synthesis of II, VII, IX, and X in pregnancy, liver dx in susceptibility
Also caused by diet, bowel dx, liver/bile dx
Vitamin K Prevent synthesis of II,
(reduced synthesis); Pregnancy (inc. clot
Antagonists VII, IX, X, proteins C, S
factors)
Fibrinolytic Agents
Anti-inflammatory, anti-
Drotrecogin Alpha Activated Protein C Sepsis
thrombotic, profibrolytic
Ionotropic Agents
Inhibits Na/K ATPase -> CHF, Atrial Nausea, vomiting, Increases automaticity
lowered intracellular K, flutter/fibrillation (slows diarrhea, visual and conduction in atrial
Digoxin
increased intracell Ca, conduction through AV disturbances, various muscle; toxic levels can
increased release of Ach node) arrythmias increase catecholamines
Tachyarrythmias (NOT Potent, but questionable
Milrinone increaes Ca influx CHF (IV)
bradycardia) efficacy
Beta 1 agonist CHF (fixed, high grade Increases CO, and
Dobutamine
(Enantiomers-some 'a') coronary occlusion) decreases VFP
Carvedilol, Reduce SNS effects in
Beta blocking activity
Metoprolol CHF
Nesiritide (Brain Activates cGMP,
CHF (IV) Is NOT arrhythmogenic
natriuretic peptide) Increases GFR
Anti-Arrythmic Drugs
Class 1A
Class 1B
Class 1C
Long-term Na blocker, Proarrythmic effects,
Propafenone
slows all conduction Granulocytosis, SLE-like
Long-term Na blocker, Life-threatening V.tach Decreased ionotropy, Oral; No anti-muscarinic
Flecainide
increased threshhold ONLY CHF, V.tach, Torsades Inc [] w/ Amiodarone
Binds to Na channels in Proarrythmias, CHF,
Moricizine No anti-muscarinic
open state (lowrs Vmax) neurologic effects, shock
Class 3
Class 4
Decrease inward Ca Reentry SV.tach, Afib, Decreases ionotropy, Contra in WPW; blocks
Verapamil current, slow AV Aflutter conversion Hypotension on cytosolic side
conduc, increase ERP,
slowed phase 4, HR Less -ionotropic
Diltiazem AV node tachycardias blocks on exterior side
slowed effects
Cholestyramine
Bile acid sequestrants - Rash, fecal impaction, Increase hepatic LDL
prevent enterohepatic constipation receptors (need
Cholestipol
recirculation (LDL now Can also bind drugs or cholesterol to make new
used to make more) vitamins --> deficiency bile acids)
Colesevelam
Stimulate guanylate Relaxes smooth muscle Headache, syncope, Tolerance after 24 hrs to
Nitroglycerin (GTN)
cyclase --> Inc. cGMP Antiplatelet; Abort MI flushing patch method
Vasodilator (arteries and Stable angina
Isosorbide dinitrate
veins) (also GTN)
Minimal reflex
Diltiazem Ca channel blocker
HTN, angina, sympathetic activation
Ca channel blocker arrythmias Headache, flushing,
Verapamil
(L type) constipation, dizziness
Ca channel blocker Prinzmetal's angina,
Nifedipine Reflex tachycardia
(dihydropyridine) HTN
Propranolol
Beta blockers
Timolol Increase diastolic time Improves subendo-
(inc. O2 supply) cardial flow, Dec HR,
Decrease Dec velocity of
Nadolol work of heart contraction
(dec. O2 demand)
Carvedilol
Antiplatelet effects
Ticlopidine See earlier
ADP antagonist
Hematopoietic Drugs
Nausea, upper
Iron Deficiency
Oral Iron supplement abdominal pain,
(Anemia)
Ferric Gluconate Liquid form(Floradix):
(Floradix) better/faster absorption
Fe Ammonium
16.5% iron
Citrate
Iron Protein Absorp. NOT affected by
Succinylate H2 antag, drugs, food
Biproduct of sugar cane
Molasses Source of iron
processing
High risk of
Iron Dextran Anaphylaxis (need test
Hemodialysis w/ EPO, dose)
Injection site rxns,
Ferric Gluconate Abnormal absorption,
IV iron supplement Diarrhea, nausea,
(Ferrlecit) intolerance to oral, oral Preferred due to less
Anaphylaxis
Iron Sucrose noncompliance adverse effects
(Venofer)
Sargramostim Recombinant GM-CFS- Chemo in AML patients Bone pain, pulmonary Pulmonary capillary leak
(Leukine) > granulocyte/macros (>55yo), BM transplant edema, heart failure --> syndrome, fever, mlaise
Filgrastim Chemo in AML patients Better tolerated than
(Neupogen) Recombinant G-CFS -> Bone pain, splenic
(>55yo), BM transplant, GM-CSF, Neulasta
neutrophils/granulocytes rupture, ARDS from
PEG-Filgrastim to prevent neutropenia prolonged action (slow
(NO macrophages) neutrophil infiltrate lung
(Neulasta) (infections) renal clearance)
PGE2 and PGI2 Vasodilation, Bronchodilation, DEC platelet agg, INC renal blood flow, GI (dec acid, inc HCO3&mucus)
Fexofenadine
(Allegra) Do NOT cross BBB
Minor Allergic reactions Little/NO sedation (NO CNS)
Loratadine (Claritin) Block H1 (edema, rash, itch), NOT antiAch
Allergic rhinitis NO motion sickness
Cetirizine (Zyrtec) help
H2 Receptor Antagonists
Cimetidine
(Tagamet)
Nizatidine (Axid)
Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous
Classification of NSAIDS
Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous
Little/NO anti-
inflammatory, Low GI, NOT an NSAID
No effect bleeding/resp Peroxides->Inactive
Not uricosuric Can affect ASA
Acetominophen Weak inhibitor of COX Analgesic, Antipyretic
Hepatic necrosis binding Greater effect
(esp. EtOH, fasting) in CNS? Free radical
Renal tubular metabolite
necrosis
Celecoxib
Selective COX-2 Contains Sulfa
(Celebrex) Osteoarthritis, Acute Gastric bleeding? Heart
Inhibitors (reversible)
pain, Menstrual pain attacks, Stroke
Rofecoxib (Vioxx) (Little effect on COX1)
Same as ASA (better for GI (N/V), CNS - dizzy, Cross sensitive ASA
Ibuprofen COX inhibitor (NSAID)
dysmenorrhea) headache, etc. Naproxen - long acting
Intractable fever Sulindac - prodrug with
COX inhibitor (Most (Hodgkins), ankylosing Frontal headache, GI less toxicity
Indomethacin
potent one) spond., OA, RA, GoutA ulcers, blood loss Contraindicated: Ulcers
close patent ductus Pregnancy, Psychiatric
Short-term analgesic Only IM NSAID
Ketorolac COX inhibitor Hepatic, renal toxicity
(compare opioids, etc) No evidence of abuse
Accumulates in synovial
Diclofenac
fluid - rapid onset
Slow-Acting Antirheumatic Drugs (SAARDs) - Disease-Modifying Antirheumatic Drugs (DMARDs)First line: NSAIDs
Decrease pain/inflammation, Dec phagocytosis of Initial Tx, or sub. for Indomethacin most
NSAIDs (NOT ASA)
urate crystals -> more excreted Colchicine common
Binds to tubulin, inhibits Acute Gout (1st line) - Reduces leukocyte
Colchicine Diarrhea, N/V
polymerization 12-24hrs till effect migration/inflammation
Inhibits Xanthine Oxids Chronic Gout (often in Prolongs T1/2 of 6-
Allopurinol Uncommon
Reduces uric acid syn. combo to start) mercaptopurine
Recombinant urate
Rasburicase Expensive
oxidase - breaks urate
GI upset, anxiety,
Theophylline Methylxanthines - PDE Reduce LT actions, Anti-inflammatory
arrhythmias, seizures
action, Ca action, Cate- Dilates, Inc work able, effects via effects on
Aminophylline cholamines, endogenus CNS stimulant, diuretic eosinophils
Caffeine
Fluticasone
Formoterol
Expectorants
Also Ipecac (subemetic
Potassium iodide Expectorants
dose)
Mucokinetic agent
Guaifenisin
Amrinone
Bronchodilation -
PDE3 inhibitors
Asthma
Enoximone
Ipopamine
Pimobendan
Verapamil
Relax bronchial SM,
Ca channel blockers
"stabilize" membranes
Nifedipine
Zarfirlukast
Leukotriene receptor Food decreases
Antagonist (nonspecific) Increase theophylline bioavailability
Montelukast and warfarin
Met. by CYP2C9,3A4
5-lipooxygenase Headache, hep. toxic
Zileuton
inhibitor Dyspepsia
Headache, viral inf.,
Omalizumab Anti-IgE monoAb SC admin only
thrombocyto, allergies
Drugs for Gastrointestinal Disorders
Peptic-acid Disorders
Omeprazole PPI Prodrug - oxidizes Zollinger-Ellison Inhibits P450; rash, hep *Acid suppression
(Prilosec) SH groups in pump syndrome DOC*, GERD enzymes, constipation (irreversible), long effect
Lansoprazole
GERD
(Prevacid)
Proton-pump inhibitors
Rabeprazole
(PPIs)
Esomeprazole &
Pantoprazole
Antidopamine - inhibits
Sulpiride NOT approved in US
gastrin release
Antidiarrheals
Kaolin Diarrhea
Thickeners and water
Kaopectate
binders
Pectin
Chlorpromazine Inhibit DA, Ach, His, and Post-op and post-rad. Works in emetic center
(Phenothiazines) alpha receptors Nausea/vomiting (oral/IV/rectal)
Dopamine receptor D2 Increases tone of
Metoclopramide GERD Diarrhea
antagonist -> inc. tone esophageal sphincter
5-HT4 agonist Nocturnal heartburn Selective availability
Cisapride
(Indirect Ach agonist) (GERD), constipation NO effect on DA system
Anticholelithics
Toxicology
Oxygen
D50W (sugar)
Initial Tx for
unresponsive patient
Thiamin
Naloxone
Fomepizole (4- NO CNS
Methanol poisoning
methylpyrazole) effects/depression
N-acetylcysteine
Acetaminophen OD
(NAC)
Desferoxamine Iron OD
Arsenic poisoning
Dimercaperol
(NOT arsine)
Polyethylene glycol Lithium, Cadmium, Fe
Whole bowel lavage
(PEG - GoLytely) poisoning
High lipids, HTN, ather- Induces CYP3A4, anti- Can cause bleeding w/
Garlic
osclerosis, Cancer thrombotic, antiplatelet surgery
Controversial
Echinacea Colds, Flu
effectiveness
Glucosamine Osteoarthritis, TMJ Does NOT affect insulin
Shellfish allergy
(sulfate) arthritis levels
(Panax) Ginseng Fatigue, "Adaptogen" Insomnia, Nervousness
Age-related macular
Lutein Carotenoid
degeneration (before)
Alzheimer Dz, Memory Interactions (CYP?), Some positive evidence
Ginkgo
enhancer, Claudication Seizures, Delayed onset for all 3 uses
Estrogenic (low) & Menopausal Sx, Breast Lymphocytopenia w/ Mech depends on
Soy
Antiestrogenic (high) Cancer certain derivative endogenous levels
Hepatotoxicity, Sedation CYP2D6 required to
Kava Anxiety (short term)
w/ other CNS depresnts metabolize
Prolonged anesthesia w/
Valerian GABA agonist Insomnia, Anxiety Additive sedation
surgery
No effect on PSA, Similar to finasteride
Saw Palmetto BPH (minor)
No impotence effectiveness
Depression (mild to 5-HT Syn. w/ SSRI's, Similar to TCA
St. John's Wort
moderate) Induces CYP effectiveness
Similar to NSAID
Chondroitin Osteorthritis Role in Prostate cz?
effectiveness
Coenzyme Q10