Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
278 Cards in this Set
- Front
- Back
- 3rd side (hint)
|
Opioid agonists
|
Codeine, Fentanyl, Heroin, Hydrocodone, Hydromorphone, Meperidine, Morphine, Methadone,Oxycodone, Oxymorphone, Propoxyphene
|
MMM
HHH OO CPF |
|
|
Mixed opioid agonists/antagonists
|
Buprenorphine, Nalbuphine, Pentazocine, Tramadol
|
T
P N B |
|
|
Opioid antagonists
|
Naloxone, naltrexone, alvimopan
|
N
N A |
|
|
Antidiarrheal opioids
|
diphenoxylate, loperamide
|
D
L |
|
|
Morphine
|
Opioid agonist, mu receptor
slow onset, 4 hr duration IV-PO adjust dose 3-5x, cont release, spinal intrathecal or epidural gluconuridation by kidney, M-6-gluconuride active metabolite |
|
|
|
Hydromorphone
|
Opioid agonist, mu receptor
IV, PO more lipid soluble, faster onset, 5x more potent than morphine less active 6-gluconuride metabolite |
|
|
|
Hydrocodone
|
Opioid agonist, mu receptor
metabolized to hydromorpohne by CYP2D6 (trade name vicodin) |
|
|
|
Oxycodone
|
Opioid agonist, mu receptor
metabolized to oxymorphone by CYP2D6 |
|
|
|
Oxymorphone
|
Opioid agonist, mu receptor
available as extended release |
|
|
|
Codeine
|
Opioid agonist, mu receptor
prodrug demethylated to morphine by CYP2D6 |
|
|
|
Propoxyphene
|
Opioid agonist, mu receptor
prodrug converted to morphine weak analgesic DO NOT USE |
|
|
|
Heroin
|
Opioid agonist, mu receptor
diacetyl morphine converted to monoacetyl morphine and morphine in brain rapid onset |
|
|
|
Methadone
|
Opioid agonist, mu receptor
oral, ultra long-acting (15-60 hrs t.5) pain, opioid addiction |
|
|
|
Meperidine
|
Opioid agonist, mu receptor
IV, PO more lipid sol, faster, 1/10 as potent as morphine hepatic metabolism to nor-meperidine (CNS stim, convulsions) serotonin syndrome |
|
|
|
Fentanyl
|
Opioid agonist, mu receptor
patch, oral, epidural |
|
|
|
Opioid agonists with active metabolites
|
morphine
hydrocodone oxycodone codeine meperidine heroin propoxyphene |
|
|
|
Opioid agonists without active metabolites
|
fentanyl
hydromorphone methadone oxymorphone |
F
H M O |
|
|
Tramadol
|
Mixed opioid agonist-antagonist
partial mu agonist and MOA uptake inhibitor moderate acute/chronic pain |
|
|
|
Pentacozine
|
Mixed opioid agonist-antagonist
kappa agonist, mu partial agonist acute short term pain (NOT chronic) also used to manage side effects |
|
|
|
Nalbuphine
|
Mixed opioid agonist-antagonist
kappa agonist, mu partial agonist acute short term pain (NOT chronic) also used to manage side effects |
|
|
|
Buprenorphine
|
Mixed opioid agonist-antagonist
mu partial agonist high affinity, kappa agonist difficult to reverse effect drug abuse and addiction |
|
|
|
Diphenoxylate
|
Antidiarrheal opioid agonist
poorly or not absorbed after oral administration |
|
|
|
Loperamide
|
Antidiarrheal opioid agonist
poorly or not absorbed after oral administration |
|
|
|
Naloxone
|
Opioid receptor antagonist
parenteral |
|
|
|
Naltrexone
|
Opioid receptor antagonist
PO |
|
|
|
Alvimopan
|
Opioid receptor antagonist
poorly absorbed orally antagonizes GI side effects of opioids |
|
|
|
General Growth Inhibitors
|
azathioprine
cyclophosphamide leflunomide methotrexate mycophenolate mofetil |
|
|
|
Glucocorticoids
|
Prednisone
|
|
|
|
mTOR inhibitors
|
Sirolimus
|
|
|
|
Calcineurin inhibitors
|
cyclosporine
tacrolimus |
|
|
|
Antibodies
|
Anti-lymphocyte globulin
Muromonab-CD3 Basiliximab Daclizumab RH(d) immune globulin |
|
|
|
Cytokines
|
Interleukin-2
IFN-gamma |
|
|
|
Adjuvants
|
BCG
|
|
|
|
BCG
|
adjuvant
live attenuated bacillus calmette-guerin increases APC activity useful in bladder cancer may cause septic shock |
|
|
|
Interleukin-2
|
cytokine
Increases proliferation of activated T cells, IFN-gamma, cytotoxic killer cells metastatic melanoma, renal cell carcinoma Shock - can be fatal |
|
|
|
IFN-gamma
|
cytokine
stimukates cell mediated IR treating severe repeated infection |
|
|
|
Cyclophosphamide
|
General growth inhibitor
cross-links DNA, kills proliferating cells used for auto-immune diseases, bone marrow transplant toxicity: myelosupression, naus/vom, infertiliity |
|
|
|
Azathioprine
|
General growth inhibitor
to 6-thioguanine - inhibits purine and DNA synthesis inactivated by xanthine oxidase (less effective with allopurinol) used for renal transplant, some autoimmune toxicity: myelosupression, naus/vom |
|
|
|
Mycophenolate mofetil
|
General growth inhibitors
hydrolized to mycophenolic acid, inhibits inosine mp dehyrogenase used for solid organ transplants, some autoimmune toxicity: myelosupression, naus/vom |
|
|
|
Methotrexate
|
General growth inhibitor
inhibits inosine and thymidine synthesis used for RA, autoimmune diseases toxicity: less myelosupression, nausea, ulcers, some hepatotoxicity |
|
|
|
Leflunomide
|
General growth inhibitor
metabolized to A77-1726 -decreases pyrimidine syntheses 19 day t.5 enterohepatic recirculation used for RA, autoimmune diseases toxicity: less myelosupression, diarrhea, some hepatotoxicity |
|
|
|
Prednisone
|
Glucocorticoid
changes transcription to reduce immune response and inflammatory response first line for organ and stem cell transplant, other inflammatory/immune disorders toxicity (long use) - Cushings, glucose intolerance, Htn, osteoporosis, immune supp, NO marrow toxicity |
|
|
|
Cyclosporine
|
Calcineurin inhibitor
prevent TCR-induced cytokine expression kidney, liver, heart transplants toxicity: nephrotoxicity, htn, hyperglycemia, liver dysfunction |
|
|
|
Tacrolimus
|
Calcineurin inhibitor
prevent TCR-induced cytokine expression 10-100X more potent than cyclosporine kidney, liver, heart transplants toxicity: nephrotoxicity, htn, hyperglycemia, liver dysfunction |
|
|
|
Sirolimus
|
mTOR inhibitor
prevents cytokine induced growth aka rapamycin solid organ transplants, GVHD in stem cell transplants antagonizes tacrolimus, synergizes with cyclosporine toxicty: profound myelosupression, hepatotoxicty |
|
|
|
Anti-lymphocyte globulin (ALG)
|
Antibody
animal derived Opsonizes T cells- prolonged T cell depletion > 1 yr toxicity: serum sickness, cytokine release syndrome |
|
|
|
muromonab-CD3
|
Antibody
mouse monoclonal blocks and opsonizes T cell receptor prolonged T cell depletion severe cytokine release syndrome, reuse limited (produces Ab response) |
|
|
|
Basiliximab
|
Antibody
anti-CD25 (IL-2 receptor) humanized blocks activated T cells moderate effect compared to ATG well tolerated |
|
|
|
Daclizumab
|
Antibody
anti-CD25 (IL-2 receptor) humanized blocks activated T cells well tolerated moderate effect compared to ATG |
|
|
|
Rh(D) immune globulin
|
human antibody
Inhibits naive Rh(D) reactive B cells given to Rh- mother to prevent hemolytic disease of newborn |
|
|
|
H1 antihistamines
|
cetirizine
dimenhydrinate diphenhydramine fexofenadine loratadine meclizine promethazine terfenadine |
1st - DDMP
2d - LCF don't use - T |
|
|
anti-TNFalpha agents
|
adalimunab
infliximab etanercept |
|
|
|
COX nonselective inhibitors
|
aspirin
diclofenac ibuprofen indomethacin ketorolac naproxen acetominaphen |
K
I A N I D A |
|
|
COX-2 selective inhibitors
|
celecoxib
rofecoxib |
|
|
|
Infliximab
|
anti-TNFalpha agent
humanized, binds TNFalpha used for RA (with methotrexate), Crohn's disease complications: increased infections |
|
|
|
Adalimunab
|
anti-TNFalpha agent
human Ab similar to inflixumab |
|
|
|
Etanercept
|
anti-TNFalpha agent
fusion protein: ligand binding domainTNFalpha receptor and human IgG Fc domain similar to inflixumab |
|
|
|
Diphenhydromine
|
H1 antihistamine (benadryl)
first generation uses: allergic rhinitis, uticaria, motion sickness marked sedation |
|
|
|
Dimenhydrinate
|
H1 antihistamine (dramamine)
first generation motion sickness marked sedation |
|
|
|
Meclazine
|
H1 antihistamine
first generation uses: allergic rhinitis, uticaria, motion sickness slight sedation |
|
|
|
Promethazine
|
H1 antihistamine
first generation uses: allergic rhinitis, uticaria, antiemetic marked sedation |
|
|
|
Loratidine
|
H1 antihistamine (Claritin)
second generation (less sedating, few anticholinergic effects) |
|
|
|
Cetirizine
|
H1 antihistamine (Zyrtec)
second generation (less sedating, few anticholinergic effects) |
|
|
|
Fenoxofenadine
|
H1 antihistamine (Allegra)
second generation (less sedating, few anticholinergic effects) |
|
|
|
Terfenadine
|
H1 antihistamine
metabolized to fenoxofenadine by CYP3A4 antibiotics and antifungals inhibit 3A4 blocks potassium channels causing lethal arrhythmias |
|
|
|
Aspirin
(acetylsalicylic acid) |
COX nonselective inhibitor
ASA to SA ASA irrev, SA rev, inhibits COX 1 and 2 antiinflammatory, antipyretic, anti-platelet (irreversible inhibits 1 week) cardiovascular prophylaxis analgesic for inflammatory pain |
|
|
|
Ketororolac
|
COX nonselective inhibitor
COX1/2: 395 post-surgical analgesic |
|
|
|
Indomethacin
|
COX nonselective inhibitor
COX1/2: 10 arthritis/antiinflammatory high incidence of intolerance (GI) |
|
|
|
Naproxen
|
COX nonselective inhibitor
OTC antiinflammatory/antipyretic Rx antiinflammatory |
|
|
|
Ibuprofen
|
COX nonselective inhibitor
OTC antiinflammatory/antipyretic |
|
|
|
Diclofenac
|
COX nonselective inhibitor
COX1/2: .3 Rx arthritis/antiinflammatory less GI irritation |
|
|
|
Diclofenac with misoprostal
|
COX nonselective inhibitor
COX1/2: .3 Rx arthritis/antiinflammatory less GI irritation prevent ulcer |
|
|
|
Acetaminophen
|
COX non-selective inhibitor
lacks effects on platelets, CV, or GI system analgesic and antipyretic effects not antiinflammatory |
|
|
|
Celecoxib
|
COX-2 selective inhibitor
(Celebrex, 10-20x COX-2 vs 1) osteoarthritis and RA lack GI, platelet, cardioprotective effects increased CV events |
|
|
|
Rofecoxib
|
COX-2 selective inhibitor
(Vioxx, 200x COX-2 vs 1) osteoarthritis and RA lack GI, platelet, cardioprotective effects increased CV events |
|
|
|
Asthma
Beta-2 adrenergic agonists |
albuterol
salmeterol salmeterol with fluticasome |
|
|
|
Asthma
Corticosteroids |
beclomethasone
budesonide fluticasone prednisone triamcinolone |
|
|
|
Asthma
Leukotrione modulators |
montelukast
zafirlukast zileuton |
|
|
|
Asthma
Degranulation inhibitors |
cromolyn
nedocromil |
|
|
|
Asthma
Muscarinic cholinergic antagonists |
ipratropium
|
|
|
|
Asthma
Miscellaneous |
omalizumab
theophylline |
|
|
|
Beclomethasone
|
Corticosteroid
aerosol inhalation long-term reduction of symptoms of asthma |
|
|
|
Budesonide
|
Corticosteroid
aerosol inhalation long-term reduction of symptoms of asthma |
|
|
|
Fluticasone
|
Corticosteroid
aerosol inhalation long-term reduction of symptoms of asthma |
|
|
|
Triamcinolone
|
Corticosteroid
aerosol inhalation long-term reduction of symptoms of asthma |
|
|
|
Prednisone
|
Corticosteroid
oral administration burst of anti-inflammatory activity for poorly controlled asthma problematic if long term |
|
|
|
Cromolyn
|
Degranulation inhibitor
inhaled powder aerosol inhibits degranulation of Mast cells, inhibits Cl channels well tolerated Only effective as long-term maintenance |
|
|
|
Nedocromil
|
Degranulation inhibitor
inhaled powder aerosol inhibits degranulation of Mast cells, inhibits Cl channels well tolerated Only effective as long-term maintenance |
|
|
|
Zileuton
|
Leukotriene modulator
synthesis inhibitor: blocks 5-lipoxygenase oral admin, long term therapy liver toxicity, inhibits CYPs |
|
|
|
Zafirlukast
|
Leukotriene modulator
LTD4 receptor antagonists can allow corticosteriod reduction oral admin, long term therapy |
|
|
|
Montelukast
|
Leukotriene modulator
LTD4 receptor antagonists can allow corticosteriod reduction oral admin, long term therapy |
|
|
|
Albuterol
|
Beta-2 adrenergic agonist
adenyl cyclase, cAMP induced bronchial smooth muscle relaxation short term relief of acute symptoms inhaled form 3-4 hours |
|
|
|
Salmeterol with fluticasone
|
Beta-2 adrenergic agonist
adenyl cyclase, cAMP induced bronchial smooth muscle relaxation long-acting 12 hrs + NOT short term relief, must be combined with corticosteroids for maintanance |
|
|
|
Ipratropium
|
Muscarinic antagonist
inhalation quaternary - no CNS effects slow acing and less efective than beta2 agonists patients intolerant of beta2agonists |
|
|
|
Theophylline
|
Miscellaneous asthma drug
methylxanthine increases cAMP, relaxes b. smooth mm oral admin, long term maintenance variable clearance rate, monitor serum levels |
|
|
|
Omalizumab
|
miscellaneous asthma drug
anti-IgE monoclonal Ab humanized mouse |
|
|
|
Volatile general anesthetics
|
desflurane
isoflurane enflurane sevoflurane nitrous oxide |
I
E D S N |
|
|
Miscellaneous anesthetic agents
|
dantrolene
succinylcholine |
|
|
|
Induction agents
|
thiopental
methohexital ketamine etomidate propofol |
M
T E P K |
|
|
Analgesics
|
alfentanil
fentanyl remifentanil sufentanil |
F
S A R |
|
|
Premedication agents
|
flumenazil
midazolam |
|
|
|
Enflurane
|
Volatile general anesthetic
metabolized 2% MAC 1.68 (use ~2.0) |
|
|
|
Isoflurane
|
Volatile general anesthetic
irritating to the airways metabolized only .2% MAC 1.15,use ~1.5% minimal myocardial depression |
|
|
|
Desflurane
|
Volatile general anesthetic
irritating to the airways metabolized only .02% MAC 7.25, use ~9.4% minimal myocardial depression prompt recovery, new, use often |
|
|
|
Sevoflurane
|
Volatile general anesthetic
non-irritating to the airways minimal myocardial deppression MAC 2.05, use ~2.7% significant metabolism at 2-5% but produces prompt recovery |
|
|
|
Nitrous Oxide
|
Volatile general anesthetic
adjunct to potent volatile MAC ~100% general anesthetics reduces MAC very insoluble minimal side effects |
|
|
|
Dantroline
|
miscellaneous anesthetic agent
treats malignant hypothermia caused by volatile anesthetics and succinylcholine |
|
|
|
Methohexital
|
Induction agent IV
barbiturate lipid soluble -rapid profound unconsciousness marked respiratory depression prompt recovery (5-8 min) no drugs to reverse decreases sympathetic brain outflow |
|
|
|
Thiopental
|
Induction agent IV
barbiturate lipid soluble -rapid profound unconsciousness marked respiratory depression prompt recovery (5-8 min) no drugs to reverse decreases sympathetic brain outflow |
|
|
|
Etomidate
|
Induction agent IV
respiratory depression no CV depression KNOW this- unique maintains BP can't be antagonized |
|
|
|
Propofol
|
Induction agent IV
unique- can be used for maintenance as well CV and Resp depression can't be antagonized least hangover |
|
|
|
Ketamine
|
Induction agent IV
NMDA receptor antagonist dissociative anesthetic sedation amnesia AND analgesia (unique) no resp/CV depression, no antagonist emergence delirium |
|
|
|
Midazolam
|
Premedication agent
benzodiazepam lipid sol, sedation and amnesia resp depression CAN be antagonized by flumazanil - unique |
|
|
|
Flumazenil
|
Premedication agent (antagonist)
antagonizes midazolam |
|
|
|
Fentanyl
|
Analgesic
useful for premedication (reduces MAC for volatile an.) potent, fast onset, shorter dur than morphine respiratory depression antagonized by naloxone |
|
|
|
Sulfentanil
|
Analgesic
premedication potent, fast, short acting opioid |
|
|
|
Alfenatil
|
Analgesic
premedication potent, fast, short acting opioid |
|
|
|
Remifentanil
|
Analgesic
premedication opioid metabolized by plasma esterase can be used as an infusion |
|
|
|
Local anesthetic esters
|
cocaine
procaine tetracaine |
C
P T |
|
|
Local anesthetic amides
|
lidocaine
mepivacaine bupivacaine prilocaine ropivacaine |
L
M B P R |
|
|
Cocaine
|
Ester local anesthetic
topical vasoconstrictor toxicity: MI, arrythmias, seizures, htn |
|
|
|
Procaine
|
Ester local anesthetic
45-60 minutes low potency |
|
|
|
Tetracaine
|
Ester local anesthetic
60-180 minute high potency |
|
|
|
Lidocaine
|
Amide local anesthetic
60-120 minutes intermediate potency |
|
|
|
Mepivacaine
|
Amide local anesthetic
90-180 minutes intermediate potency |
|
|
|
Bupivacaine
|
Amide local anesthetic
240-180 minutes high potency |
|
|
|
Prilocaine
|
Amide local anesthetic
60-120 min |
|
|
|
Ropivacaine
|
Amide local anesthetic
180-30 min |
|
|
|
Tricyclic antidepressants
|
amitriptyline
amoxapine imipramine nortriptyline |
|
|
|
Serotonin reuptake inhibitors
|
citalopram
escitalopram fluoxetine sertraline |
|
|
|
Atypical antidepressants
|
bupropion
mirtazapine nefazodone venlafaxine |
|
|
|
MAO Inhibitors
|
phenelzine
selegiline tranylcypromine |
|
|
|
Bipolar Treatment
|
lithium
carbamazepine valproic acid |
|
|
|
Stimulants
|
amphetamine
atomoxetine dextro-amphetamine methylphenidate modafinil |
|
|
|
Amitriptyline
|
tricyclic antidepressant
nonspecific monoamine reuptake inhibitor (NE, 5HT) lots of side effects - also block muscarinic, adrenergic, and histamine receptors |
|
|
|
Amoxapine
|
tricyclic antidepressant
nonspecific monoamine reuptake inhibitor (NE, 5HT) lots of side effects - also block muscarinic, adrenergic, and histamine receptors |
|
|
|
imipramine
|
tricyclic antidepressant
nonspecific monoamine reuptake inhibitor (NE, 5HT) lots of side effects - also block muscarinic, adrenergic, and histamine receptors |
|
|
|
nortriptyline
|
tricyclic antidepressant
nonspecific monoamine reuptake inhibitor (NE, 5HT) lots of side effects - also block muscarinic, adrenergic, and histamine receptors |
|
|
|
citalopram
|
SSRI
safer,few antimuscarinic effects, no cardiotoxicty block some p450s, eliminated via kidneys |
|
|
|
escitalopram
|
SSRI
safer,few antimuscarinic effects, no cardiotoxicty block some p450s, eliminated via kidneys |
|
|
|
fluoxetine
|
SSRI
safer,few antimuscarinic effects, no cardiotoxicty block some p450s, eliminated via kidneys |
|
|
|
Sertraline
|
SSRI
safer,few antimuscarinic effects, no cardiotoxicty block some p450s, eliminated via kidneys |
|
|
|
Bupropion
|
atypical antidepressant
inhibits dopamine reuptake useful for rapid cycling bipolar disorder |
|
|
|
Venlafaxine
|
atypical antidepressant
serotonin and norepinephrine reuptake inhibitor |
|
|
|
Nefazodone
|
atypical antidepressant
inhibits serotonin reuptake and blocks 5-HT receptors |
|
|
|
Mirtazipine
|
atypical antidepressant
increases NE release by blocking alpha2 receptors |
|
|
|
Phenelzine
|
MAOI
irreversible, long acting increases concentrations of NE, 5-HT, DA third line severe, unpredictable side effects avoid tyramine |
|
|
|
Tranylcypromine
|
MAOI
irreversible, long acting increases concentrations of NE, 5-HT, DA third line severe, unpredictable side effects avoid tyramine |
|
|
|
Selegiline
|
REVERSIBLE, long acting MAO-B inhibition (DA)
Parkinson's increases concentrations of DA avoid tyramine |
|
|
|
Lithium
|
bipolar treatment
maintenance eliminated by kidneys toxic, low theraputic index CNS, CV, thyroid, renal, teratogenic effects diabetes insipidus interacts with thiazides diretics and NSAIDS |
|
|
|
Carbamazepine
|
bipolar treatment
anticonvulsant toxic |
|
|
|
Valproic acid
|
Bipolar treatment
anti-convuslant side effects |
|
|
|
Amphetamine
|
stimulant (Adderall)
ADHD, narcolepsy increases release of DA and NE in brain MAO inhibitor, increased vesicular (VMAT) and non-vesicular release (DAT, NAT) CNS, CV, GI effects addiction potential |
|
|
|
Atomoxetine
|
stimulant (Strattera)
ADHD NE reuptake inhibitor NOT psychostimulant, not habit forming, not controlled |
|
|
|
Dextro-amphetamine
|
stimulant (Dexedrine)
ADHD, narcolepsy Oral admin, absorbed, metabolized liver, urine excr. drug of abuse |
|
|
|
Methylphenidate
|
stimulant (Ritalin)
narcolepsy, ADHD oral admin, high conc in brain |
|
|
|
Modafinal
|
Stimulant
Narcolepsy fewer psychoactive, euphoric effects |
|
|
|
Benzodiazepines
|
diazepam
chlordiazepoxide alprazolam oxazepram triazolam lorazepam temazepam midazolam flumazenil (antagonist) |
D
C L O A T M T shortest |
|
|
Barbituates
|
pentobarbital
phenobarbital amobarbital thiopental |
|
|
|
Miscellaneous sedatives
|
meprobamate
chloral hydrate buspirone zolpidem zaleplon |
|
|
|
Diazepam
|
Benzodiazepine
long acting (>24 hrs) anxiety, withdrawal, muscle relaxant physical dependence, tolerance potential |
|
|
|
Chlordiazepoxide
|
Benzodiazepine
long acting (>24 hrs) anxiety, withdrawal, muscle relaxant metabolized in liver by p450s physical dependence, tolerance potential |
|
|
|
Alprazolam
|
Benzodiazepine
intermediate acting (2-6 hrs) insomnia, anxiety physical dependence, tolerance potential |
|
|
|
Lorazepam
|
Benzodiazepine
intermediate acting (6-24 hrs) insomnia, anxiety, muscle relaxant physical dependence, tolerance potential |
|
|
|
Oxazepam
|
Benzodiazepine
intermediate acting physical dependence, tolerance potential |
|
|
|
Triazolam
|
Benzodiazepine
short acting physical dependence, tolerance potential |
|
|
|
Midazolam
|
Benzodiazepine
ultra-short acting (<2 hours) physical dependence, tolerance potential |
|
|
|
temazepam
|
Benzodiazepine
physical dependence, tolerance potential |
|
|
|
Flumazenil
|
Benzodiazepine antagonist
|
|
|
|
Phenobarbital
|
Barbiturate
long acting (80-120 hrs) anticonvulsant CV, resp depression binds to p450s, induces drug metabolizing activity |
|
|
|
Pentobarbital
|
Barbiturate
intermediate acting (15-50 hrs) preop sedation CV, resp depression binds to p450s, induces drug metabolizing activity |
|
|
|
Amobarbital
|
Barbiturate
Short acting (10 hrs) preop sedation CV, resp depression binds to p450s, induces drug metabolizing activity |
|
|
|
Thiopental
|
Barbituate
ultra short acting (3-10 hrs) anesthesia induction CV, resp depression binds to p450s, induces drug metabolizing activity |
|
|
|
Buspirone
|
miscellaneous antianxiety
partial 5HT receptor only antianxiolytic, no CNS depression no dependence 1-3 weeks for onset |
|
|
|
Zolpidem
|
miscellaneous hypnotic
BZ binding site in GABA receptor peak level within 1-2 hours after oral admin induces sleep, decrease latent onset insomnia |
|
|
|
Zaleplon
|
miscellaneous hypnotic
BZ binding site in GABA receptor peak level within 1-2 hours after oral admin induces sleep, decrease latent onset insomnia |
|
|
|
Anticonvulsants
|
carbamazapine
ethosuxamide gabapentin lamotigine phenobarbitol phenytoin valproic acid pregabalin topiramate zonisamide clonazepam diazepam lorazepam |
|
|
|
Partial simple epilepsy
|
Preferred: phenytoin, carbamazepine, lamortigine
Alternative: phenobarbital, primidone, gabapentin |
|
|
|
Partial complex epilepsy
|
Preferred: phenytoin, carbamazepine, lamortigine
Alternative: primidone, gabapentin |
|
|
|
Generalized tonic-clonic epilepsy
|
Preferred: phenytoin, carbamazepine, lamortigine
Alternative: phenobarbital, primidone, valproic acid |
|
|
|
Generalized absence epilepsy
|
Preferred: ethosuxamide
Alternative: clonazepam, valproic acid |
|
|
|
Generalized myoclonic epilepsy
|
Preferred: clonazepam, valproic acid
Alternative: lamortigine |
|
|
|
Generalized febrile seizures
|
Preferred: phenobarbital
Alternative: primidone |
|
|
|
Generalized status epilepticus
|
Preferred: phenytoin, diazepam
Alternative: phenobarbital |
|
|
|
Phenytoin
|
Antiepileptic
drug of choice for adults. oral, IV for emergency not used for absence seizures blocks voltage activated Na+ and Ca2++ channels enhances p450 system adverse: CNS, GI, rash, megaloblastic anemia, teratogen |
|
|
|
Carbamazepine
|
Antiepileptic
drug of choice for partial simple, partial complex, tonic-clonic blocks voltage activated Na+ channels enhances p450 system adverse: CNS, GI, liver toxicity, aplastic anemia, teratogen |
|
|
|
Valproic acid
|
Antiepileptic
drug of choice for myoclonic seizures blocks voltage gated Na+ and Ca2++ channels adverse: liver failure, GI, CNS,alopecia, rash, thrombocytopenia, teratogen inhibits phenobarbital metabolism |
|
|
|
Ethosuximide
|
Antiepileptic
drug of choice for absence seizures blocks t-typ Ca2++channels in thalamic neurons adverse: GI,CNS,thrombocytopenia, aplastic anemia, SYSTEMIC LUPUS |
|
|
|
Phenobarbital
|
Antiepileptic, barbiturate
simple partial, recurrent tonic-clonic and febrile seizures combined with carbamazepine and phenytoin for smaller doses facilitate activation of GABA receptors safer. adverse: CNS, GI, rashes |
|
|
|
diazepam
|
Antiepileptic, benzodiazepine
acute tx of status epileptius IV potentiate GABA activation safer. CNS, tolerance |
|
|
|
lorazepam
|
Antiepileptic, benzodiazepine
acute tx of status epileptius IV potentiate GABA activation safer. CNS, tolerance |
|
|
|
Clonazepam
|
Antiepileptic, benzodiazepine
myoclonic and absence seizures potentiate GABA activation safer. CNS, tolerance |
|
|
|
Lamotrigine
|
Antiepileptic
simple or complex partial, tonic-clonic seizures inhibits glutamate release blocks voltage activated Ma channels Metabolized in liver, halflife inc by enzyme inducing drug, increased by valproic acid |
|
|
|
Gabapentin
|
Antiepileptic
simple or complex partial, tonic-clonic seizures enhances GABAergic transmission? not metabolized, does not induce hepatic enzymes short half life (5-8 hr) does not bind plasma proteins |
|
|
|
Pregabalin
|
Antiepileptic
simple or complex partial seizures blocks Ca channels, glutamate release drowsiness, dizzy, weight gain, rash |
|
|
|
Topiramate
|
Antiepileptic
simple or complex partial, tonic-clonic seizures blocks Na channels, increases postsynaptic GABA r drowsiness, dizzy, ataxia weight loss, rash |
|
|
|
Zonisamide
|
Antiepileptic
simple, complex partial and tonic clonic seizures blocks Na channels, T-type Ca channels drowsiness ataxia, confusion, vomit, rash |
|
|
|
Phenothiazine antipsychotics
|
chlorpromazine
fluphenazine thioridazine |
|
|
|
Butyrophenone antipsychotics
|
haloperidol
|
|
|
|
Atypical antipsychotics
|
clozapine
olanzapine risperidone |
|
|
|
Thioxanthene antipsychotics
|
thiothixene
|
|
|
|
Chlorpromazine
|
Phenothiazine antipsychotic
D2 receptor antagonist lots of bad side effects |
|
|
|
Fluphenazine
|
Phenothiazine antipsychotic
D2 receptor antagonist lots of bad side effects |
|
|
|
Thioridazine
|
Phenothiazine antipsychotic
D2 receptor antagonist lots of bad side effects |
|
|
|
Thiothixene
|
Thioxanthene antipsychotic
D2 receptor antagonist lots of bad side effects |
|
|
|
Haloperidol
|
Butyrophenone antipsychotic
D2 receptor antagonist lots of bad side effects |
|
|
|
Clozapine
|
Atypical antipsychotic
D2 receptor antagonist no dry mouth induces weight gain more selective, fewer extrapyramidal effects, no prolactin elevation |
|
|
|
Olanzapine
|
Atypical antipsychotic
D2 receptor antagonist induces weight gain more selective, fewer extrapyramidal effects, no prolactin elevation |
|
|
|
Risperidone
|
Atypical antipsychotic
D2 receptor antagonist induces weight gain more selective, fewer extrapyramidal effects, no prolactin elevation |
|
|
|
Typical antipsychotic side effects
|
cholinergic muscarinic receptor block (dry mouth, blurred vision, const, urinary ret, confusion, memory impairment)
alpha-adenoreceptor block pituitary D2 receptor block - increased prolactin release - infertility and impotence Histamine receptor block: sedation and weight gain Striatal dopamine receptor block: parkinsonian effects, dystonias |
|
|
|
Enhancers of DA synthesis
|
levodopa (L-DOPA)
L-DOPA+ carbidopa entacapone amantadine |
|
|
|
Dopamine receptor agonists
|
apomorphine
bromocriptine pramipexole ropinirole |
|
|
|
Anticholnergics (antiparkinson)
|
benztropine
trihexyphenidyl |
|
|
|
MAOb inhibitors
|
rasagiline
selegiline |
|
|
|
Acetylcholinesterase inhibitors
|
donepizil
galantamine rivastigmine tacrine |
|
|
|
NMDA antagonist
|
memantine
|
|
|
|
Levodopa
|
enhances DA synthesis
L-DOPA DA precurser, crosses BBB less effective after 3-5 years most is metabolized periphally short half-life (1-2 hr) Side effects: nausea, vom, arrhythmias, hypotension, dyskinesia, mood, hallucinations |
|
|
|
Levidopa + Carbidopa
|
enhances DA synthesis
carbidopa blocks peripheral metabolism of L-DOPA, more available in brain allows lower dose, fewer side effects Side effects: nausea, vom, arrhythmias, hypotension, dyskinesia, mood, hallucinations |
|
|
|
Entacapone
|
enhances DA synthesis
inhibits catechol-o-methyltransferase with levidopa/carbidopa further increases availability in brain Parkinson's |
|
|
|
Amantidine
|
enhances DA synthesis
alleviates bradykinesia and rigidity for mild to moderate disease inc DA release, blocks cholinergic and glutaminergic NMDA receptors |
|
|
|
Selegiline
|
MAOb inhibitor
decrease DA catabolism limits H2O2 byproduct adjunct to levodopa metabolized to methamphetamine & amphetamine |
|
|
|
Rasagiline
|
MAOb inhibitor
Parkinson's decrease DA catabolism adjunct to levodopa not metabolized to amphetamines |
|
|
|
Bromocriptine
|
Dopamine receptor agonist
D2 agonist, D1 partial early Parkinson's monotherapy, later adjunct begin low and gradually increase dose CV, CNS, GI side effects contraindicated if heart or mental problems |
|
|
|
Ropinirole
|
Dopamine receptor agonist
D2 and D3 agonist early monotherapy, later adjunct begin low and gradually increase dose CV, CNS, GI side effects contraindicated if heart or mental problems |
|
|
|
Pramipexole
|
Dopamine receptor agonist
D2 and D3 agonist early monotherapy, later adjunct begin low and gradually increase dose CV, CNS, GI side effects contraindicated if heart or mental problems |
|
|
|
Apomorphine
|
Dopamine receptor agonist
acute tx of advanced patinets for off periods subQ NOT IV (thrombus, PE) nausea, vom, arrhythmia,hallucinations, sleepiness |
|
|
|
Trihexyphenidyl
|
muscarinic antagonist
alleviate parkinson tremor and rigidity muscarinic side effects: dry mouth, constipation.... also delirium, psychosis, memory impairment |
|
|
|
Benztropine
|
muscarinic antagonist
alleviate parkinson tremor and rigidity muscarinic side effects: dry mouth, constipation.... also delirium, psychosis, memory impairment |
|
|
|
Donepezil
|
AChE inhibitor
70 hr half-life modest improvement in some Alzheimer's patients p450 metabolism safe. sympathetic side effects. |
|
|
|
Galantamine
|
AChE inhibitor
7 hr half-life modest improvement in some Alzheimer's patients p450 metabolism safe. sympathetic side effects. |
|
|
|
Rivastigmine
|
AChE inhibitor
1.5 hr half-life modest improvement in some Alzheimer's patients metabolized by the plasma cholinesterase safe. sympathetic side effects. |
|
|
|
Tacrine
|
AChE inhibitor
3 hr half-life modest improvement in some Alzheimer's patients HEPATOTOXICTY p450 metabolism sympathetic side effects. |
|
|
|
Memantine
|
NMDA receptor antagonist
protects neurons from Ca overload Alzheimer's improved daily life and functioning additive benefits with donepizil side FX: dizziness, headaches, confusion, agitation |
|
|
|
Carbonic anhydrase inhibitors
|
acetazolamide
methazolamide dichlorphenamide |
|
|
|
Thiazides and Thiazide-like
|
chlorothiazide
hydrochlorothiazide hydroflumethiazide metolazone trichlomethiazide |
|
|
|
Loop agents
|
bumetanide
ethacrynic acid furosamide torsemide |
|
|
|
K+ sparing agents
|
amiloride
eplerenone spironolactone triamterene |
|
|
|
Osmotic agents
|
glycerin
mannitol |
|
|
|
Acetazolamide
|
Carbonic anhydrase inhibitors
proximal tubule leave NaHCO3 in urine (inc pH) Urine ions: increase Na, K, HCO3, H2PO4 potassium wasting based on sulfanilimides (sulfa allergy) glaucoma, altitude sickness, counteracting diuretic alkalosis Adverse: metabolic acidosis, kidney stones, worsen hepatic encepalopathy, bmdepression |
|
|
|
Methazolamide
|
Carbonic anhydrase inhibitors
proximal tubule leave NaHCO3 in urine (inc pH) Urine ions: increase Na, K, HCO3, H2PO4 potassium wasting based on sulfanilimides (sulfa allergy) glaucoma, altitude sickness, counteracting diuretic alkalosis Adverse: metabolic acidosis, kidney stones, worsen hepatic encepalopathy, bmdepression |
|
|
|
Dichlorphenamide
|
Carbonic anhydrase inhibitors
proximal tubule leave NaHCO3 in urine (inc pH) Urine ions: increase Na, K, HCO3, H2PO4 potassium wasting based on sulfanilimides (sulfa allergy) glaucoma, altitude sickness, counteracting diuretic alkalosis Adverse: metabolic acidosis, kidney stones, worsen hepatic encepalopathy, bmdepression |
|
|
|
Glycerin
|
osmotic diuretic
suppos/IV primary loop of henle, secondary prox conv tubule draw water into blood, wash out medullary gradient potassium wasting all ions except hydrogen increased out of urine (everything follows water out) |
|
|
|
Mannitol
|
osmotic diuretic
IV only reduce brain swelling primary loop of henle, secondary prox conv tubule draw water into blood, wash out medullary gradient potassium wasting all ions except hydrogen increased out of urine (everything follows water out) |
|
|
|
Osmotic diuretic indications
|
Acute renal failure
acute tubular necrosis dialysis disequilibrium syndrome acute glaucoma reduce brain swelling |
|
|
|
Osmotic diuretic adverse events
|
pulm cong to pulmonary edema
hyponatremia not for anuria, impaired liver function NOT id active intracranial bleeding glycerin may cause hyperglycemia |
|
|
|
Furosemide
|
Loop Diuretic (Lasix)
unique: weak carbonic anhydrase inhibitor, gluconuridated in kidney, increases systemic venous capacitance ihibit Na/K/Cl symporter in TAL ions stay in TAL, water stays with them potassium wasting all ions increased |
|
|
|
Buteminide
|
Loop Diuretic
ihibit Na/K/Cl symporter in TAL ions stay in TAL, water stays with them potassium wasting all ions increased |
|
|
|
Ethacrynic acid
|
Loop Diuretic
ihibit Na/K/Cl symporter in TAL ions stay in TAL, water stays with them potassium wasting all ions increased |
|
|
|
Torsemide
|
Loop Diuretic
ihibit Na/K/Cl symporter in TAL ions stay in TAL, water stays with them potassium wasting all ions increased |
|
|
|
Loop diuretic indications
|
acute pulmonary edema
CHF Htn (thiazides preferred) Nephrotic syndrome Edema and ascites of cirrhosis chronic renal failure |
|
|
|
Loop diuretic adverse reactions
|
well tolerated in general
hyponatremia hypokalemia ototoxicity sulfa allergy interacts w/other drugs |
|
|
|
Hydrochlorothiazide
|
Thiazide diuretic
t.5=2.5 hrs block NaCl symport not K distal collecting tubule potssium wasting moderately efficacious all ions except Ca and Mg increased in urine |
|
|
|
Chlorothiazide
|
Thiazide diuretic
t.5=1.5 hrs block NaCl symport not K distal collecting tubule potssium wasting moderately efficacious all ions except Ca and MG increased in urine |
|
|
|
Hydroflumethiazide
|
Thiazide diuretic
t.5= 17 hrs block NaCl symport not K distal collecting tubule potssium wasting moderately efficacious all ions except Ca and MG increased in urine |
|
|
|
Trichlormethiazide
|
Thiazide diuretic
t.5= 2.3-7.3 hours block NaCl symport not K distal collecting tubule potssium wasting moderately efficacious all ions except Ca and Mg increased in urine |
|
|
|
Metolazone
|
Thiazide-LIKE diuretic
does not decrese renal blood flow, used for renal disease block NaCl symport not K distal collecting tubule potssium wasting moderately efficacious all ions except Ca and MG increased in urine |
|
|
|
Thiazide diuretic indications
|
Htn - no risk of hypovolemia
CHF edema safer calcium reabsorption is increased - tx osteoporosis unknown why treatment of nephrogenic diabetes insipidus reduces urine |
|
|
|
Thiazide diuretic adverse effects
|
volume depletion, hyponatremia, metabolic acidosis
sulfa allergies increases effects of anesthetics NSAIDS decrease effectiveness rare CNS/GI effects ED |
|
|
|
Amiloride
|
K sparing
inhibitor of renal Na channels DCT and CD used to block K excretion combined with other diuretics urine ions: (inc Cl,Na; decrease K, H, Ca, Mg) eliminated by kidney |
|
|
|
Triamterine
|
K sparing
inhibitor of renal Na channels DCT and CD used to block K excretion combined with other diuretics urine ions: (inc Cl,Na; decrease K, H, Ca, Mg) eliminated by liver |
|
|
|
Inhibitors of Renal Na Channels indications
|
enhance thiazide and loop diuretic effects and reduce K loss
Liddle's syndrome aerosol in CF |
|
|
|
Inhibitors of renal Na channels adverse events
|
hyperkalemia - arrhythmia & death
megaloblastic anemia in cirrhosis |
|
|
|
Spironolactone
|
Mineralocorticoid antagonists
Potassium sparing DCT and CD stop retention of salt and water by comp binding mineralocorticoid receptor urine ions: inc Na, Cl; decreased K, H, Mg |
|
|
|
Eplerenone
|
Mineralocorticoid antagonists
Potassium sparing DCT and CD stop retention of salt and water by comp binding mineralocorticoid receptor urine ions: inc Na, Cl; decreased K, H, Mg |
|
|
|
Mineralocorticoid antagonists indications
|
coadministered with thiazides and loop diuretics for potassium sparing action
spironolactone: promary hyperaldosteronism, ascites and edema from cirrhosis |
|
|
|
Mineralocorticoid antagonists adverse reactions
|
hyperkalemia
salicylates decrease efficiency feminization GI/CNS |
|
|
|
Antidiuretics
|
chlorpropamide
desmopressin lypressin vasopressin |
|
|
|
Uricosuric agents
|
probenecid
sulfinpyrazone |
|
|
|
Miscellaneous anti-gout
|
alllopurinol
colchicine |
|
|
|
Vasopressin
|
Antidiuretic drug
aka ADH (arginine or lysine form) binds V1 receptors Stimulates water reabs by increasing aquaporins in in DT and CD |
|
|
|
Desmopressin
|
Antidiuretic drug
synthetic arginine vasopressin analog little V1 activity Stimulates water reabs by increasing aquaporins in in DT and CD |
|
|
|
Antidiuretic drug indications
|
diabetes insipidus
|
|
|
|
Antidiuretic drug adverse effects
|
coronary artery constriction
nasal mucosa drying |
|
|
|
Chlorpropamide
|
Antidiuretic drug
sulfonurea increases ADH secretion prev used for type II diabetes |
|
|
|
Probenecid
|
uicosuric agent
stops gout organic acid transporter competitive antagonist in PT (initial) and DT (long term) |
|
|
|
Sulfinpyrazone
|
uricosuric agent
stops gout organic acid transporter competative antagonist in PT (initial) and DT (long term) |
|
|
|
Allopurinol
|
Stops gout
inhibits xanthine oxidase (and thus stops uric acid formation) |
|
|
|
Colchicine
|
Stops gout
acts on neutrophils which carry uric acid crystals to joints |
|
