Q1 Drugs/vaccines

Front 1

Tacrolimus/ cyclosporine

Back 1

Inhibit calcineurin

Inhibition of IL-2 production in T-cells

Front 2

Rapamycin

Back 2

Inhibits mTOR

Inhibition of IL-2 receptor signaling cascade
Inhibits t-cell proliferation

Front 3

Morphine/ Codeine

Back 3

Substrate for CYP 2D6

Morphine undergoes some first pass metabolism
Codeine becomes morphine (active) through O-dealkylation
Codeine is metabolized by CYP 2D6

Effects of codeine are diminished in poor metabolizers
Patients with hyperactive CYP 2D6 can have codeine/morphine toxicity

Front 4

Fluvoxamine

Back 4

CYP 1A2 inhibitor

Increases the half-life of tizandine because it blocks CYP 1A2

Front 5

Tizandine

Back 5

CYP 1A2 substrate

Has a longer half-life when given with fluvoxamine (CYP 1A2 inhibitor)
Side effects include drop in BP/sedation

Front 6

Dextromethorphan

Back 6

CYP 2D6 substrate

Used to measure CYP 2D6 activity (hyperactive in 30% east Africans and absent in 7% caucasians)

Front 7

Disulfiram

Back 7

Aldehyde dehydrogenase inhibitor

Also inhibits CYP 2E1
Causes buildup of acetaldehyde in ethanol metabolism (undesirable effects)

Front 8

Allopurinol

Back 8

Xanthine oxidase inhibitor

Prevents the formation of uric acid in gout

Front 9

Warfarin

Back 9

Anticoagulant

Inhibition of Vitamin K
Metabolized by CYP 2C9

Front 10

Tamoxifen

Back 10

CYP 2D6 substrate

Usually, metabolized to endoxifen - this does not occur when CYP 2D6 is inhibited

Front 11

Papain

Back 11

Cleaves Ig into 2 Fab and 1 Fc region

Acts on the hinge region above disulfide bonds
Keeps the hinge region connected to the Fc region

Front 12

Pepsin

Back 12

Cleaves Ig into F(ab')2 and pFc' region (cut up)

Acts on the hinge region below the disulfide bonds
Keeps the hinge region connected to the F(ab')2 region

Front 13

Venom from black widow spider

Back 13

Blocks Ach action

Lipase which breaks up the Ach nerve terminal

Front 14

Bochilinous toxin

Back 14

Blocks the calcium influx transporters at the presynaptic terminal

Blocks Ach release from the nerve terminal
Most toxic chemical on a mg/mg basis - sold as BOTOX

Front 15

Snake venom

Back 15

Ach ANTAgonist

Stops respiration

Front 16

Muscarine

Back 16

Poision which activates muscarinic Ach receptors

Acts on CV system/glands/smooth muscle

Front 17

Methacoline

Back 17

Ach muscarinic (M2) agonist (NOT nicotinic)

Acts on Heart/CV Sytstem
Longer duration than Ach, not as easily degraded
Used in asthma challenge test (causes bronchoconstriction)

Front 18

Carbachol

Back 18

Ach muscarinic (low dose) and nicotinic (high dose) agonist

Acts in Eyes (Canal of Schlemm) - indicated for Glaucoma
Not easily degraded by Cholinesterase; longer duration than Ach

Front 19

Bethanecol

Back 19

Ach muscarinic agonist

GI System - used after GI surgery to promote motility - long duration of action

Front 20

Nicotine

Back 20

Ach nicotinic agonist

Nicotinic receptors (ganglia, Adrenal gland, NMJ)

Front 21

Atropine

Back 21

Ach muscarinic ANTAgonist (Competitive)

Acts on all muscarinic receptors (does not discriminate)
N has 3 bonds, so it is a neutral molecule: can get into the brain

Front 22

Scopolamine

Back 22

Ach muscarinic ANTAgonist

Acts on Muscarinic receptors
Treats motion sickness, nausea, vomiting

Front 23

Homatropine

Back 23

Ach muscarinic ANTAagonist

Acts in eyes (dilation)
Short-acting, used by ophthamologists

Front 24

Ipratropium

Back 24

Ach muscarinic ANTAagonist

Bronchi/bronchioles (dilation)
Quaternary nitrogen (charged)

Front 25

Tiotropium

Back 25

Ach muscarinic ANTAagonist

Bronchi/bronchioles (dilation)
Quaternary nitrogen (charged)

Front 26

Tolterodine

Back 26

Ach muscarinic ANTAgonist

Bladder retention
Can cause systemic effects, so use with care

Front 27

D-Tubocurarine

Back 27

Ach nicotinic (submuscular) ANTAgonist

NMJ
Used to paralyze muscles during surgical procedures

Front 28

Hexamethonium

Back 28

Ach nicotinic (subneuronal) ANTAgonist

Blocks adrenal gland/ganglia - lowers BP
Used for hypertensive crisis
Also blocks PNS systemically, causing harsh side effects

Front 29

Trimethaphan

Back 29

Ach nicotinic (subneuronal) ANTAgonist

Blocks adrenal gland/ganglia - lowers BP
Used for hypertensive crisis
Also blocks PNS systemically, causing harsh side effects

Front 30

Mecamylamine

Back 30

Ach nicotinic (subneuronal) ANTAgonist

Blocks adrenal gland/ganglia - lowers BP
Used for hypertensive crisis
Also blocks PNS systemically, causing harsh side effects

Front 31

Physostigmine

Back 31

AchE inhibitor (Class I - carbamate)

Steric hindrance
Tertiary compoind (can cross the BBB), not used anymore

Front 32

Neostigmine

Back 32

AchE inhibitor (Class I - carbamate) - reversible

Steric hindrance
Used for myesthenia gravis
Quaternary compound
Taken orally, but has slow absorption rate, used in surgery

Front 33

Pyridostigmine

Back 33

AchE inhibitor (Class I - carbamate)

Steric hindrance
Used for myesthenia gravis
Quaternary compound
Taken orally, but has slow absorption rate

Front 34

Rivastigmine

Back 34

AchE inhibitor (Class I - carbamate)

Steric hindrance
Used for Alzheimer's (stabilization)
Given in a patch form (because patients may forget to take the correct dosage at the correct time)
Tertiary compound (cross the BBB)

Front 35

Donepezil (aricept)

Back 35

AchE inhibitor (Class I - carbamate)

Steric hindrance
Used for Alzheimer's (stabilization)
Tertiary compound to cross BBB

Front 36

Edrophonium

Back 36

AchE inhibitor (Class II) - reversible

Shortest acting cholinesterase inhibitor
Quaternary compoind, used as a diagnostic for myesthenia gravis, used in surgery along with neostigmine

Front 37

Echothiophate

Back 37

AchE inhibitor (Class III - organophosphate) - irreversible

Acts in eyes - treat glaucoma (like carbachol) long-acting
Long-duration of action drug
Be careful when putting echothiophate into the eyes

Front 38

Parathion

Back 38

AchE inhibitor (Class III - organophosphate) - irreversible

Insecticide - crop dusting
Converterd to paraoxon in the body

Front 39

Malathion

Back 39

AchE inhibitor (Class III - organophosphate) - irreversible

Insecticide - common household
Converted to malaoxon, human liver is able to destroy malaoxon to protect us

Front 40

Sarin

Back 40

AchE inhibitor (WMD)

Most potent man-made WMD
Very lipid soluble
Build up Ach everywhere
Bronchoconstriction/bronchial secretions
Shut down the cardiac and respiratory centers

Front 41

Soman

Back 41

AchE inhibitor (WMD)

Very lipid soluble
Build up Ach everywhere
Bronchoconstriction/bronchial secretions
Shut down the cardiac and respiratory centers

Front 42

Tabun

Back 42

AchE inhibitor (WMD)

Very lipid soluble
Build up Ach everywhere
Bronchoconstriction/bronchial secretions
Shut down the cardiac and respiratory centers

Front 43

Vx

Back 43

AchE inhibitor (WMD)

Very lipid soluble
Build up Ach everywhere
Bronchoconstriction/bronchial secretions
Shut down the cardiac and respiratory centers

Front 44

MARC 1-kit

Back 44

Atropine (Ach muscarinic receptor ANTAgonist) + Pralidoxime (nucleophile)

Antidote for gas poisoning
Atropine: can partially offset cardiac/respiratory center malfunction
2-PAM is a highly nucleophilic drug

Front 45

Norepinephrine

Back 45

Alpha-1/2, Beta-1/3 agonist

NT for SNS
Vasoconstriction at systemic blood vessels, to the GI system
Contraction to get dilation of the eyes
Contraction of the bladder sphincter to maintain urine
Lipolysis
Increased contractility of the heart
Increased HR
Increased renin secretion in the kidney to increase blood volume

Front 46

Epinephrine

Back 46

Alpha-1/2, Beta-1/2/3 agonist

Sympathetics and BETA-2 receptors
Vasoconstriction at systemic blood vessels, to the GI system
Contraction to get dilation of the eyes
Contraction of the bladder sphincter to maintain urine
Vasodilation to the skeletal muscle and liver
Increased potassium uptake for skeletal muscle
Increased glycogenolysis at the liver
Lipolysis
Increased contractility of the heart
Increased HR
Uterine muscle relaxation
Bronchodilation

Front 47

Dopamine

Back 47

D1 agonist (and partial beta-1 agonist in the heart)

Dilates renal blood vessels

Front 48

Clonidine

Back 48

Alpha-2a/c agonist

Rostroventrolateral medulla (RVLM)
Causes inhibition of NE release, treats HTN, Tourret's and withdrawl abuse from drugs

Front 49

Theophylline/ Aminophylline

Back 49

Non-selctive PDE-4 inhibitor

Bronchial smooth muscle (for asthma)
Increases vasodilation

Since it is nonspecific, it can increase contractility in the heart as a side effect (not good for asthma patients since heart will demand more oxygen)
Increases histone acetylation (depresses inflammatory response)
Affects adenosine receptors

Front 50

Reserpine

Back 50

VMAT inhibitor

Acts on VMAT in dopaminergic/noradrenergic nurons
Blocks transport of dopamine (catecholamines) into vesicles
No longer used to treat HTN and schizophrenia
More selective drugs discovered
Caused profound depression
Irreversibly blocks VMAT (affects serotonin also)

Front 51

Isoproterenol

Back 51

Selective beta-1/2 agonist

Acts on Heart/CV System
Increases contractility/HR without affecting mean BP (systolic BP increases but diastolic BP decreases)
Causes vasodilation of arteries

Front 52

Phenylephrine

Back 52

Alpha-1 agonist

Blood vessels (vasoconstriction)
Increases TPR/BP
Nasal decongestant
Decreases HR

Front 53

Phentolamine

Back 53

Alpha-1/2 ANTAgonist

Blood vessels (causing vasodilation)
Blocks high doses of EPI from causing vasoconstriction of alpha receptors

Front 54

Metyrosine

Back 54

Tyrosine hydroxylase inhibitor

TH in catecholaminergic neurons
Not widely used
Used before treatment of pheochromocytomas to reduce amount of catecholamines present before/after surgery

Front 55

L-DOPA

Back 55

Substrate for aromatic L-AA decarboxylase

Effects in Catecholaminergic neurons
Bypasses the rate-limiting step of catecholamine synthesis

Front 56

L-DOPA?????

Back 56

?????Uncouples VAMPs and SNAPs (used for vesicular exocytosis)

Presynaptic membrane
Does not allow vesicular Ach release from presynaptic terminal
Known as BOTOX
Used for muscle spasticity disorder

Front 57

Amphetamine

Back 57

MAO, VMAT and uptake inhibitor

Presysnaptic terminal
Increase release of NE, dopamine and serotonin
Used for ADD, narcolepsy, general stimulant

Front 58

Tyramine

Back 58

Increases NE release

Presynaptic terminal
Product of bacterial degradation of tyrosine in the gut
found in many aged foods

Front 59

Ephedrine

Back 59

Increases NE release and beta-receptor agonist

Presynaptic terminal
Can be converted to methamphetamine (abused drug)
Similar to tyramine
Causes bronchodilation, stimulates heart, raises BP

Front 60

Cocaine

Back 60

Uptake inhibitor

Presynaptic membrane (uptake)
In the periphery, cocaine blocks only the NET
In the brain, it blocks serotonin, dopamine and NE uptake

Front 61

Despiramine

Back 61

NET selective inhibitor

Stronger NET blocker than amphetamines

Front 62

Trycyclic antidepressants

Back 62

NET selective inhibitor

Stronger NET blocker than amphetamines

Front 63

Phenelzine

Back 63

MAO inhibitor

Allows for increased NE and reversal of uptake pump

Front 64

Sildenafil

Back 64

Selective PDE-5 inhibitor

Targets PDE-5 (bronchi) - used for asthma
Decreases pulmonary HTN/ARDS
Increase cerebral blood flow
Also causes increased male erection
Increases NO release from NANC nerves to increase cGMP

Front 65

Terbutaline/ Albuterol

Back 65

Selective beta-2 agonist

Lungs (for asthma)
Stimulates the heart as well (like isoproterenol), but not as much
Overuse causes resistance/desensitization

Front 66

Dobutamine

Back 66

Selective beta-1 agonist

(for heart failure)
Not used chronically because it has to be infused
Racemic (+ and - form)
Stronger inotropic vs. chronotropic effect
Can cause downregulation/desensitization over time

Front 67

Ritodrine

Back 67

Selective beta-2 agonist

Causes relaxation of the pregnant uterus to allow baby to develop longer

Front 68

Alpha-methyldopa

Back 68

Alpha 2 agonist

CNS (and periphery to some extent)
At low doses, given orally,does not stimulate peripheral receptors, but still can affect the CNS
Inhibition of NE
Also used for withdrawal signs from opiates

Front 69

Propranolol

Back 69

Non-selective beta receptor ANTAgonist

Heart (blocks EPI action)
Metabolized by liver, so we have to give a higher dose orally than through IV

Decreases HR, and thus, BP
In HTN, decreases CO
In angina, it causes less use of oxygen by heart
Stabilize heart in cardiac arrhythmias
In chronic heart failure, decreases chance for arrhythmia and prevents remodeling of heart;

Front 70

Metropolol

Back 70

Selective beta-1 ANTAgonist

Heart (blocks EPI action)
Decreases HR, and thus, BP
In HTN, decreases CO
In angina, it causes less use of oxygen by heart
Stabilize heart in cardiac arrhythmias
In chronic heart failure, decreases chance for arrhythmia and prevents remodeling of heart

Front 71

Atenolol

Back 71

Selective beta-1 ANTAgonist

Heart (blocks EPI action)
NOT used in renal insufficiency b/c it is metabolized in the kidney
In HTN, decreases HR and BP, decreasing CO
In angina, it causes less use of oxygen by heart
Stabilize heart in cardiac arrhythmias
In chronic heart failure, decreases chance for arrhythmia and prevents remodeling of heart

Front 72

Pindolol

Back 72

Beta-1 ANTAgonist and partial beta-2 agonist

Heart (blocks EPI action in times of stress)
Maintains resting HR, but decreases stressed HR

Front 73

Tamulosin

Back 73

Alpha-1a ANTAgonist

Prostate
Used for BPH
Dilates prostatic vessels

Front 74

Prazosin

Back 74

Alpha-1a, b and d ANTAgonist

Blood vessels; Treats HTN

Front 75

Phenoxybenzamine

Back 75

Alpha-1/2 ANTAgonist (irreversible)

Blood vessels; Treats HTN

Front 76

Carvedilol

Back 76

Alpha-1 ANTAgonist AND beta-ANTAgonist

Used for heart failure
Blocks alpha-1 receptors responsible for heart thickening/remodeling; has anti-proliferative properties

Front 77

Labetalol

Back 77

Alpha-1 ANTAgonist AND beta-ANTAgonist

Used for heart failure
Blocks alpha-1 receptors responsible for heart thickening/remodeling; has anti-proliferative properties