Term
| verapamil; type? action? use? SEs? |
|
Definition
non-selective (cardiac vs. vascular) L-type CaCB
decreases HR and O2 Uses - supraventricular arrhythmia SEs - constipation, edema, increased digoxin levels |
|
|
Term
| Nifedipine; type? action? T1/2? |
|
Definition
vascular L-type CaCB
lower blood pressure
arteriole vasodilator - decreases afterload
3-4hr, halflife |
|
|
Term
| Diltiazem; type? action? use? |
|
Definition
L-type CaCB
Decreases HR and 02 demand
Use - coronary artery vasospasm |
|
|
Term
|
Definition
T-type CaCB
Use - absanes petite mal seizures |
|
|
Term
|
Definition
T-type CaCB
use - absence (petit mal) seizures |
|
|
Term
|
Definition
antiseizure
T-type CaCB
Mixed mode of action (MOA) drug |
|
|
Term
|
Definition
T-type CaCB
anti-seizure
Mixed mode of action (MOA) drug |
|
|
Term
|
Definition
T-type CaCB (NaCB and CaCB)
anti-seizure med
CYP 3A4 inducer
SEs - gum hyperplasia, Hirsuitism, folate deficiency, megaloblastic anemia, rash, peripheral neuropathy |
|
|
Term
| pregabalin and gabapentin |
|
Definition
Ca channel blocker at alpha-2-delta subunit
(or N-type/NPQR)
reduce NT release
use - chronic pain |
|
|
Term
|
Definition
Ryanodine Receptor blocker
inhibits release of intracellular Ca from skeletal muscle sarcoplasmic reticulum
use- malignant hyperthermia |
|
|
Term
|
Definition
barbiturate like
i.v. sedative, hypnotic (induces anesthesia)
short duration of action |
|
|
Term
|
Definition
"vigorous GABA transaminase inhibitor"
anti-epileptic
inhibits GABA transaminase - increases GABA |
|
|
Term
|
Definition
anti-epileptic
GABA-reuptake inhibitor - increases GABA |
|
|
Term
|
Definition
GABA-B agonist (presynaptic)
reduces NT release
reduce muscle tone in people w/ spacticity |
|
|
Term
|
Definition
used for chronic pain (marketed as antiseizure)
Acts on alpha-2 delta subunit of Ca-channel
recudes Ca and therefore NT release |
|
|
Term
|
Definition
used for chronic pain
acts on Alpha-2 delta subunit of Ca-channel
Reduces Ca and therefore NT release |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
Long acting BDZ
Rohypnol (date rape drug) |
|
|
Term
|
Definition
| ultra-short acting non-BDZ hypnotic |
|
|
Term
|
Definition
| short acting non-BDZ hypnotic |
|
|
Term
|
Definition
Lunesta
longer acting non-BDZ hypnotic |
|
|
Term
|
Definition
BDZ antagonist, used for BDZ overdose
Can induce seizures and panic attacks, especially in pt's dependent on BDZ
does not work for non-BDZ hypnotics |
|
|
Term
|
Definition
Barbiturate
Sedative-hypnotic (anesthesia)
can cause release of Histamine -> pseudoalergic reaction |
|
|
Term
|
Definition
Barbiturate
anti-epileptic |
|
|
Term
|
Definition
Aspirin
irreversible inhibitor of COX
good in low doses
SEs - aspirin asthma, rye syndrome, NSAID SEs |
|
|
Term
| acetyc acid/phenylacetic acid |
|
Definition
|
|
Term
|
Definition
NSAID
a pheylacetic acid
favored by orthopedics |
|
|
Term
|
Definition
NSAID
a heterocyclic acetic acid
very potent i.v. administered, used in anesthesia |
|
|
Term
|
Definition
|
|
Term
|
Definition
COX II inhibitor
only one still on the market |
|
|
Term
| Acetaminophen/Paracetamol; what causes toxicity? |
|
Definition
antipyretic and mild analgesic
NOT an anti-inflammatory - no peripheral COX inhibition
-GSH deficiency prevents conversion of toxic metabolite to nontoxic -> liver necrosis |
|
|
Term
|
Definition
used for acetaminophen overdose to ensure enough GSH in liver
*must give with alpha-1 agonist to combat vasodilation |
|
|
Term
|
Definition
same mode of action as acetaminophen
antipyretic, STRONG analgesic, NO anti-inflammatory effect
Relaxes smooth muscle - spasmolytic effect, good for kidney and gallbladder stones
-if given in i.v. bolus can cause serious drop in BP |
|
|
Term
|
Definition
NSAID
LOX inhibitor
indicated for asthma
only one in USA |
|
|
Term
|
Definition
D2 blockers
"azines"
interact w/ many receptors so many SEs
-H1 - sedation/weight gain
-Mblocker - dry mouth, medriasis, bronchial dilation, tachycardia, constipation, urine retention
-D2 blocker - extrapyramidal SEs
-Alpha blocker - hypotension
-torsades |
|
|
Term
|
Definition
D2 blockers
use - pruritis, motion sickness, sedative
"coast guard cocktail" - for motion sickness |
|
|
Term
|
Definition
D2 blocker
use - drug induced nausea and migraine |
|
|
Term
|
Definition
D2 blocker
antipsychotic
used for long term treatment |
|
|
Term
|
Definition
D2 blockers
more D2 specific than phenothiazines and non-trycyclic |
|
|
Term
|
Definition
D2 blocker - butryphenone
very selective for D2
EPS; dystonic reaction, akinesia, rigidity, tremors, akathisia and tarditive dyskinesia |
|
|
Term
|
Definition
anticholinergic
anti-parkinson agent
SE - dystonia |
|
|
Term
|
Definition
anticholinergic
anti parkinsonian agent |
|
|
Term
|
Definition
antihistamine and anticholinergic
anti-parkinsonian agent |
|
|
Term
|
Definition
antiviral
anti-parkinson agent |
|
|
Term
|
Definition
atypical antipsychotic
Low D2, high D4 affinity and 5HT2 antagonist
CYP 1A2 metabolism
SE - agranulocytosis, hypersalivation and hyperthermia, seizures, weight gain (10x10), trycyclic effects |
|
|
Term
|
Definition
atypical antipsychotic
5HT2 antagonist > D2 antagonist (also D4 affinity
CYP 1A2 metabolism
SEs - (clozapine w/ NO agranulocytosis) hypersalivation, hyperthermia, seizures, weight gain, trycyclic effects |
|
|
Term
|
Definition
atypical antipsychotic
5HT2 antagonist >>>D2 antagonist & NaSRI
3A4 metabolism
SE - QT prolongation -> torsades |
|
|
Term
|
Definition
atypical antipsychotic
D2 antagonist = 5HT2 antagonist
3A4 metabolism
SEs - sedation, cataracts and hypothyroidism |
|
|
Term
|
Definition
5HT2 antagonist, 5HT 1A partial agonist, D2 partial agonist,
2D6/3A4 metabolism
Less weight gain |
|
|
Term
|
Definition
DA receptor agonist, Ergotamine derivative
Parkinson Disease |
|
|
Term
|
Definition
DA receptor agaonist, non-ergotamine derivative
Parkinson Disease |
|
|
Term
|
Definition
DA receptor agonist, non-ergotamine derivative
Parkinson Disease |
|
|
Term
|
Definition
COMT inhibitor (prevents inactivation of levodopa in brain)
Parkinson diseease tx |
|
|
Term
|
Definition
| inhibits DDC, allowing levodopa to go to brain |
|
|
Term
| Stabilizing levodopa (Stalevo) |
|
Definition
| carbidopa, levodopa, and entacapone |
|
|
Term
|
Definition
1st generation H1 blocker
alkylamine |
|
|
Term
|
Definition
1st generation H1 blocker
ethanolamine |
|
|
Term
|
Definition
1st genration H1 blocker
ethanolamine |
|
|
Term
|
Definition
1st generation H1 blocker
used in "coast guard cocktail"
phenothiazine |
|
|
Term
|
Definition
1st generation H1 blocker
piperazine |
|
|
Term
|
Definition
1st generation H1 blocker
piperazine |
|
|
Term
|
Definition
| 2nd generation H1 blocker |
|
|
Term
|
Definition
| 2nd generation H1 blocker prodrug - CYP 3A4 -> fexofenadine |
|
|
Term
|
Definition
| 2nd generation H1 blocker |
|
|
Term
|
Definition
| 2nd generation H1 blocker prodrug -CYP 3A4 -> Carebastin |
|
|
Term
|
Definition
| 2nd generation H1 blocker |
|
|
Term
|
Definition
| 3rd generation H1 blocker |
|
|
Term
|
Definition
| 3rd generation H1 blocker |
|
|
Term
|
Definition
3rd generation H1 blocker
longest t1/2 |
|
|
Term
|
Definition
| 3rd generation H1 blocker |
|
|
Term
|
Definition
H2 blocker
first available, interacted w/ CYP enzymes and made action of other drugs unpredictable |
|
|
Term
|
Definition
|
|
Term
|
Definition
VW class III and non-selective beta-blocker
ventricular and supra ventricular arrhythmias
torsades de pointes |
|
|
Term
| Amiodarone, class? use? SEs |
|
Definition
Class X (mixture of class I-IV)
anti-arrhythmic (most efficacious)
MANY side effects (thyroid, neurologic, opthalmic, etc) and long half-life, PK favors toxicit |
|
|
Term
|
Definition
VW class X, anti-arrhythmic
Less toxic Amiodarone, shorter T1/2 |
|
|
Term
| Sulfonyl-urea agents; action? SEs? examples? |
|
Definition
hypoglycemic agents
pancreatic K-channel blockers -> increased inslulin release
0rally administered
can't use in Type I DM
all have "gl" in name
SEs - increased wight and decreased GLU
glibenclamid, glyburide, glipizid, glimepririd |
|
|
Term
| Metformin, use? action? byproduct? |
|
Definition
Non-Sulfonyl-urea hypoglycemic agent (don't know how it works)
One of the best drugs for diabetes control
Inhibits lactate uptake and hepatic GNG via AMP-kinase
Byproduct - guanidine |
|
|
Term
|
Definition
Non-Sulfonyl-urea insulin release
end in "-glinid"
Rapid onset, short action
less hypoglycemia and weight gain than SUs |
|
|
Term
| Nicorandil, action? use?, SEs? |
|
Definition
K-channel opener
arterial relaxation (decreased afterload) also stimulates cGMP -> relax venous smooth muscle (decreased preload)
tx of angina, congestive heart failure, HTN
SEs - oral ulcerations |
|
|
Term
|
Definition
K-channel opener
dilate arteries -> increased 02 and nutrient supply -> hair growth! |
|
|
Term
| carbemazipine; type? channel? SEs (and cause)? |
|
Definition
Anti-epileptic
Na channel blocker - membrane stabilization
CYP P450 3A4 inducer
SEs (similar to TCA)
sedation - H1 receptorblocker
dry mouth - M-receptor blocker
arrhythmia Na and K channel blocker
hypotension - alpha-R blocker
weight gain - 5-HT |
|
|
Term
| Phenytoin; type? channel? SEs? |
|
Definition
anti-epileptic Na and Ca channel blocker
CYP 3A4 inducer
0 order kinetics
SEs - gum hyperplasia, megaloblastic anemia, folate/B12 deficiency, peripheral neuropathy, skin rash, hirsuitism |
|
|
Term
|
Definition
Na channel blocker
LA ester |
|
|
Term
| lidocaine; channel? type? |
|
Definition
Na channel blocker
LA amide and VW Class IB anti-arrhythmic |
|
|
Term
| quinidine; action? type? SEs? |
|
Definition
Na channel blocker
VW Class IA anti-arrhythmics
atropine-like effects (anticholinergic)
SEs - cinchonism (blurred vision, tinnitus, headaches) increased digoxin leves, N & V, arrhythmia |
|
|
Term
| procainamide; action? type? |
|
Definition
"VW class IA"
 technically it is a VW IC (Na blocker only) but is metabolized to NAPA, a VW class III (K-blocker)
*fast metabolizers at higher risk for torsades de pointes |
|
|
Term
| flecainide; action? type? |
|
Definition
Na channel blocker
VW class IC anti-arrhythmic |
|
|
Term
| Ketamine; active isomer? action? effect? SEs? |
|
Definition
(S) esketamine
NMDA antagonist
potent analgesic; Sympathomimetic = increased RR, HR, BP, O2 consumption
SEs - bronchorrhea, sialorrhea, vivid dreams |
|
|
Term
| Memantine; action? use? SEs |
|
Definition
NMDA antagonist
rapid blocking/unblocking (unlike Mg)
prevention of dementia/improved mental performance
SE - bradycardia and bronchoconstriction |
|
|
Term
| methadone; action? PK? effect? |
|
Definition
1/2 NMDA antagonist and 1/2 mu-agonist
slow onset and long t1/2
analgesia and sedation |
|
|
Term
| lamotrigine; use? action? |
|
Definition
anti-epileptic
glutamate release inhibitor and Na-channel blocker |
|
|
Term
|
Definition
anti-epileptic
NMDA antagonist and GABA agonist |
|
|
Term
| Topiramate; use? action? SEs |
|
Definition
anti-epileptic
AMPA antagonist and GABA agonist
weight loss (from reduced DA release)inhibits carbonic anhydrase - makes soda taste bad, and impaired memory
"california drug" or "stupimax" |
|
|
Term
| morphine, receptor? effects? metabolism/t1/2? |
|
Definition
mu-receptor
supraspinal/spinal analgesia, euphoria, respiratory depression, bradycardia, obstipation, urinary retention, miosis,
+itching (Histamine release)
+emesis (DA)
do not need liver for metabolism
t1/2 = 3hrs |
|
|
Term
| Piritramid, receptor? effect? potency |
|
Definition
mu-receptor
morphine w/ less side effects (less histamine)
analgesic potency = 0.8 |
|
|
Term
| codeine, activation? potency? |
|
Definition
metabolized to 10% morphine by P450 3A4
AP = 0.1 |
|
|
Term
|
Definition
P450 2D6 -> mu-agonist (chronic pain)
NaSRI -> chronic pain
central alpha-2 agonist -> decreased NT and inhibits sympathetic NS (clonidine like) |
|
|
Term
| pentazocine, receptor? effect? |
|
Definition
kappa-agonist (only one)
weak mu-agonist
spinal analgesia, causes dysphoria, psychomimetic effects |
|
|
Term
| methodone, receptor? onset/t1/2? |
|
Definition
mu-agonist and NMDA antagonist
slow onset 6-8hrs
long t1/2 = 55hrs |
|
|
Term
|
Definition
| morphine, alfentanil, fentanyl, remifentanil, sufentanil |
|
|
Term
|
Definition
| i.v. administered opiod, ultrashort t1/2 - need constant infusion |
|
|
Term
| meperidine/pethidin, action? use? t1/2? interactions? |
|
Definition
anticholinergic, SSRI, alpha blocker (vasodilation), medriasis,
postanesthetic shivering
short t1/2
Interaction with MAO-I |
|
|
Term
|
Definition
| 5HT-3 blockers, antiemetic |
|
|
Term
|
Definition
muscarin blocker, antiemetic
transdermal
only treats emesis from motion sickness |
|
|
Term
|
Definition
| D2 antagonist, antiemetic |
|
|
Term
|
Definition
| D2 antagonist, anti-emetic |
|
|
Term
|
Definition
fibric acid derivatives
all end in -fibrate EXCEPT gemfibrizol
activate PPAR-alpha
main effect - Decrease TGs
SEs - when combined w/ statins -> rhabdomyolysis -> renal failure |
|
|
Term
| -glitazones, effect? SEs? benefits? |
|
Definition
thiazolidinediones
activate PPAR-gamma
Tx of Type II DM - improved sensitivity to insulin
some affinity for PPAR alpha, so also decrease TGs
SEs - edema and heart failure
*do not cause hypoglycemia (like SUs and repaglinide), but slow onset |
|
|
Term
|
Definition
| same as human insulin w/ 1 aa substitution pts can eat w/in 10 mins of administration TO: .25-1hr, D: 3-5hrs |
|
|
Term
|
Definition
same as human insulin w/ 1 aa transposition
more rapidly absorbed subcutaneously than human insulin
TO: .25-.5 hrs, D: 4-6hrs |
|
|
Term
|
Definition
soluble insulin
made with zinc
only type used i.v. (for life threatening hyperkalemia)
TO: .5-1hr, D: 6-10hrs |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
tx for myelocytic leukemia (MCL)
blocks ATP binding site on BCR-ABL tyrosine kinase, preventing autophosphorylation and activation
Mut at T315l (imatinib binding domain) confers resistance to imatinib, dasitinib and nilotinib |
|
|
Term
|
Definition
EGFR inhibitor
Tx of non-small cell lung cancer
less nausea than previous chemotherapy |
|
|
Term
|
Definition
EGFR inhibitor
non-small cell lung cancer and pancreatic cancer |
|
|
Term
|
Definition
| Chimeric (mouse/human) monoclonal antibody against EGFR |
|
|
Term
|
Definition
non-selective inib
targets many RTK |
|
|
Term
|
Definition
non-selective inib
targets many RTK |
|
|
Term
|
Definition
non-selective inib
targets many RTK |
|
|
Term
|
Definition
5HT-1A agonist
also alpha-1 adrenergic antagonist
used for hypertension |
|
|
Term
| Buspirone, action? onset? use? |
|
Definition
5HT-1A agonist, moderate D2 affinity, 5HT-2 agonist
onset 4-6 weeks, months for full effect
chronic anxiety |
|
|
Term
|
Definition
| MAO-A and B inhibitor - antidepressant |
|
|
Term
|
Definition
| MAO-A and B inhibitor - anti-Parkinsons |
|
|
Term
|
Definition
5HT-2 antagonist and H1 antagonist
migraines |
|
|
Term
|
Definition
5HT-2 antagonist
anxiety and depression |
|
|
Term
|
Definition
5HT-2 antagonist
anxiety and depression |
|
|
Term
|
Definition
5HT2 antagonist and alpha1-blocker
hypertension, Raynaud's (spasm of femoral artery) |
|
|
Term
|
Definition
| 5HT2 antagonist and SSRI antidepressant off market - liver damage |
|
|
Term
|
Definition
5HT2 and SSRI
antidepressent
still on market |
|
|
Term
|
Definition
5HT2 antagonist and D2 blocker (equally)
antipsychotic |
|
|
Term
|
Definition
5HT2 antagonist > D2 blocker
antipsychotic |
|
|
Term
|
Definition
5HT2 antagonist >>> D2 blocker & NaSRI
antipsychotic
risk of torades |
|
|
Term
|
Definition
atypical antipsychotic
5HT2 antagonist and 5HT-1A agonist
no weight gain or risk of torsades |
|
|
Term
|
Definition
5HT3 antagonist
extremely long acting
given i.v. once before each cycle of chemotherapy |
|
|
Term
| metoclopramide; action, use, SEs |
|
Definition
5HT-4 agonist, D2 agonist, 5HT-3 antagonist, cholinesterase inhibitor
anti-nausea and vomiting
tarditive dyskinesia |
|
|
Term
|
Definition
5HT-4 agonist
use: gastroparesis
off market - interfered with K-channel blockers -> torsades |
|
|
Term
|
Definition
5HT-4 agonist
essentially cisapride w/o K-blockage |
|
|
Term
|
Definition
NaSRI
chronic pain and antidepressant
essentially a tricyclic antidepressant without the SEs |
|
|
Term
| 11-beta hydroxysteroid dehydrogenase 2 |
|
Definition
Converts cortisol to cortisone in the kidney
Prevents overactivation of MC receptors
Is inhibited by licorice -> pseudohyperaldosteronism |
|
|
Term
|
Definition
mineralocorticoid
AIE/MCE = 10/125 |
|
|
Term
|
Definition
mineralocorticoid
AIE/MCE = 0/20 |
|
|
Term
|
Definition
glucocorticoid, short acting
AIE/MCE = 1/1 |
|
|
Term
|
Definition
glucocorticoid, short acting
AIE/MCE = 0.8/0.8 |
|
|
Term
|
Definition
glucocorticoid, intermediate acting
AIE/MCE = 4/0.3 |
|
|
Term
|
Definition
glucocorticoid, intermediate acting
AIE/MCE = 4/0.8 |
|
|
Term
|
Definition
glucocorticoid, intermediate acting
AIE/MCE = 5/0.5 |
|
|
Term
|
Definition
glucocorticoid, intermediate acting
AIE/MCE = 5/0 |
|
|
Term
|
Definition
glucocorticoid, long acting
AIE/MCE = 35/0 |
|
|
Term
|
Definition
glucocorticoid, long acting
AIE/MCE = 30/0 |
|
|
Term
|
Definition
glucocorticoid, long acting
AIE/MCE = 10/0 |
|
|
Term
|
Definition
inhaled steroid
used for asthma |
|
|
Term
|
Definition
inhaled steroid
used in asthma and COPD |
|
|
Term
|
Definition
inhaled steroid
used in asthma
10% bioavailability |
|
|
Term
|
Definition
inhaled steroid
used in asthma
20-30% bioavailability - tell patients to wash out mouth after inhalation |
|
|
Term
|
Definition
| inhibitor of steroid synthesis |
|
|
Term
|
Definition
| inhibitor of steroid synthesis |
|
|
Term
|
Definition
inhibitor of steroid synthesis
antifungal |
|
|
Term
|
Definition
inhibitor of steroid synthesis
anti-progesterone |
|
|
Term
|
Definition
inhibitor of steroid synthesis
blocks aldosterone, reduces BP |
|
|
Term
|
Definition
inhibitor of steroid synthesis
blocks aldosterone, reduces BP |
|
|
