Pharm Sheet

8/12/2019 Pharm Sheet

1/14

Drug Effect Characteristics

Epinephrine

SNS NT catecholamine -

all alpha and beta

receptor stimulation

increase HR, constrict blood vessels,

dilate vessels to skeletal muscle and

liver, bronchodilator. Used for

Anaphylaxis

Norepinephrine

SNS NT catecholamine -

alpha1/2 and beta 1 fight or flight

Metyrosine

Inhibitor of Tyrosine

Hydroxylase

Inhibits production of all catecholamines

- used in pheochromocytoma where

making excess epi and nor epi

L-Dopa

Precursor to

catecholamine synthesis

Bypasses the RLS and can cross the

BBB easier than dopamine so given as a

therapy for parkinson's disease allowing

brain to make dopamine easier. SNS

side effects throughout body though.

Tyramine

naturally occuring MAO

compound found in foods

that acts as

catecholamine releasing

agent

large intake with MAO inhibitors -

hypertensive crisis

Amphetamine

Indirect General Agonist

CNS stimulant. Releases

stored catecholamines

facilitates release of NE, Epi, DA. Also

blocks reuptake and blocks degradation

by MAO. Used for ADHD and narcolepsy.

High abuse potential - more potent than

cocaine which only blocks reuptake.

Causes tolerance.

Ephedrine


Releases stored

Catecholamines.

Activates alpha and beta

receptors and increases

catecholamine release

release of Ne into nerve terminal andweakly stimulates beta receptors =

bronchodilation, increased hr, increased

bp. Found in weight loss drugs and

nasal decongestants. Tolerance

develops. Starting material for synthesis

of methamphetamine.

Cocaine


Serotonin/epinephrine/no

repinephrine/dopamine

reuptake inhibitor

increases catecholamines in the synapse

so have greater affect. Can cross BBB

and cause addiction by affecting the

mesolimbic reward pathway.

Desipramine

Tri cyclic Norepinephrine

reuptake inhibitor

used as a tri-cyclic anti-depressant,very selective (Only NE) and potent,

also used for ADHD (underproduction of

norepinephrine has been associated

with ADHD). Does not cause tolerance

because only blocks NE (DA causes

tolerance). Also causes cardiac

arrhythmias.


2/14

Selegiline/Phen

elzine

Selective Inhibitor of

MAO-B

because of slectivity, MAO-A can still

continue to metabolize tyramine so

fewer food-drug interactions.

Aminophylline

Competitive non-

selective

phosphodiesterase

(normally removes cAMP

in cell) inhibitor

Increases cAMP leading to

brochodilation (use is for asthmatics

that are also on beta blockers for HTN

treatment so can't use albuterol) - less

potent and shorter acting than

theophylline. But are non-specific so

also get increased heart rate (which

consumes o2) and contactility (other

effects of increased cAMP - D and beta

receptors). not used.

Theophylline

Competitive non-

selective

phosphodiesterase

inhibitor

Increases cAMP leading to

brochodilation (use is for asthmatics

that are also on beta blockers so can't

use albuterol)

Sildenafil (AKA

viagra) Selective PDE-5 inhibitor

increases cGMP which is only found in

certain tissues - smooth muscle in penis

relaxes allowing for erection. Also

decreses resistance in lungs (for

pulmonary HTN) and increases cerebral

blood flow.

Isoproterenol

non selective beta

adrenergic agonist - beta

1 and 2

used for bradychardia/heart block to

increase contractility. Can also be used

for asthma to bronchodilate but not

used for this much

Dopamine

D1 Receptor Agonist

D1>beta1>alpha1

low dose = increase blood flow to

kidneys. Higher dose = beta1 effects =increase hr and contractility. High dose

= include vasoconstriction. Use in shock

to increase CO via beta1 and preserve

kidney function via D1

Dobutamine

Primarily B1 Receptor

Agonist

increases contractility with no real

change in heart rate. Inotropic. Used to

treat acute but potentially reversible

heart failure

Albuterol Beta 2 selective agonist

leads to bronchodilation via increase in

cAMP - use in asthmatics, inhaled.

Ritodrine Beta 2 selective agonist

leads to bronchodilation, also used toprevent premature uterine

contractions(good to prevent delivery

before fetal respiratory tract developed)

Propanolol

Non-selective beta

blocker decrease CO


3/14

Metoprolol beta1 selective blocker

Treatment of diseases such as

hypertension. Greater exercise tolerance

because beta2 receptors can still

mediate vasodilation. Also

glycogenolysis is less impeded so better

for diabetics.

Pindolol weak beta blocker

Treatment of diseases such as

hypertension. Doesn't slow heart rate as

much but still blocks increase in HR and

CO produced by SNS stimulation so less

likely to cause severe bradychardia in

pts with htn and low hr (athletes). So

better for exercise tolerance.

Carvedilol alpha1 and beta blocker

blocking beta = decreased CO and

blocking alpha = vasodilation. So used

to treat htn. Decreases

mortality/morbidity in pts with heart

failure. Also decreases size of heart wall

and is antioxidant

Labetalol alpha1 and beta blocker used to treat htn in pregnancy.

Phenylephrine selective alpha 1 agonist

causes vasoconstriction of nasal blood

vessels = decongestant, dilates pupil,

increases bp and decreases hr via

baroreceptor reflex. Given as a nasal

spray reduces the systemic side effects

on bp and hr. extended use = rebound

hyperemia and ischemia.

Clonidine

alpha 2a agonist in the

brain

decreases SNS output (NE release) =

decreased bp - used for htn, touretts

syndrome, and drug withdrawal. Works

within the CNS. Can also stimulate post

synaptic alpha 2 receptors causing

vasoconstriction but this is only at high

doses (also why better given orally over

IV). over time the lack of SNS

stimulatio will increase the receptors so

if suddenly go off the drug then htn will

be very bad. is physiologiceffect.Application for hypertension

(especially with renal disease)

Brimonidine

Alpha 2 adrenergic

agonist

Vasoconstriction of blood vessels

leading to reduction in aqueous humor

flow. Lowering of intraocular pressure in

patients with glaucoma or ocular

hypertension.


4/14

Phentolamine Alpha1 antagonist Anti-hypertensive.

Phenoxybenzam

ine

Non-selective Irreversible

Alpha antagonist

noncompetitive/irreversible. Alkylates

receptors (including serotonin and

histamine). Not used much. Only to

block catecholamine affects before

surgery to remove pheochromocytoma

Prazosin Alpha1 antagonist

anti-hypertensive. Better than

phentolamine because less reflexive

tachycardia. Orthostatic htn with first

dose though.

Tamsulosin Alpha1 antagonist

treatment of BPH because causes

relaxation of smooth muscle of prostate,

trigone muscle of bladder, and urethra.

Less orthostatic hypotension because is

1A selective.

"-olol" Beta Antagonist suffix

"-terol" Beta 2 Agonist suffix

Aspirin

SALICYLATE: Analgesic

and Anti-inflammatory

Characteristics:

Acetaminophen

Analgesic only (use in

asthmatics, kids,

pregnant women)Characteristics:

Ibuprofen

PROPRIONIC ACID:

Analgesic and Anti-

inflammatory

Characteristics:

Naproxen

PROPRIONIC ACID:

Analgesic and Anti-

inflammatory

Characteristics:

Ketoprofen

PROPRIONIC ACID:

Analgesic and Anti-

inflammatory

Characteristics:


5/14

Diflunisal

SALICYLATE: Analgesic

and Anti-inflammatory

Characteristics:

Sulindac

ACETIC ACID: Anti-

Inflammatory Only

Characteristics:

Indomethacin

ACETIC ACID: Anti-

Inflammatory Only

Characteristics:

Celecoxib/Celeb

rex

COX2 INHIBITOR: Anti-

Inflammatory Only: black

box

Characteristics:

Rofecoxib

COX2 INHIBITOR:

Analgesic and Anti-

inflammatory: Removed

from market

Cortisol

ec :

Short ActingGlucocorticoid (8-12

hours)

Characteristics:


6/14

Cortisone

Short Acting

Glucocorticoid (8-12

hours)

Characteristics:

Fludrocortisone

Mineralocorticoid (8-12

hours)

Characteristics:

Prednisone

Short Acting


hours)

Characteristics:

Triamcinolone

Intermediate Acting


hours)

Characteristics:

Dexamethasone

Long lasting


hours)

Characteristics:

Aminoglutethimi

de

Anti-Steroid

Characteristics:

Blocks initial step of

Metyrapone

ec :

Anti-Steroid

Characteristics:

Tests the capacity of HPA


7/14

Pentobarbital

Effect:

Barbiturate - General

CNS depressant: depress

heart rate, lower bp,

depress respiration

Characteristics:

High GABA affinity but

also blocks calcium and

AMPA receptorssedation

side effects = not used.

Very long t1/2 - 40

hours, knocks patients

out for days

Thiopental

Effect:




depress respiration

Characteristics:

Highly lipophilic -

absorbed quick but

duration of action short.

Induction agent.

Phenobarbital

Effect:




depress respiration

Characteristics:

Used as anti-seizure:

increase GABA affinity =cl channels open longer.


8/14

Vincristine

Effect:

Targets Mitotic Spindle

Characteristics:

Prevents polymerization

of microtubules. TX: HL

Paclitaxel

Effect:

Targets Mitotic Spindle

Characteristics:

Enhances microtubule

formation. TX: Breast CA

(in addition to CMF)

Cyclophosphami

de

Effect:

Alkylating/DNA Cross-

linking

Characteristics:

Pro-Drug: metabolized by

P450 into phosphoramide

mustard (cytotoxic) and

acrolein (causes cystitis).

Co administer with

MESNA to decrease

cystitis side effect.

Decrease in WBC somonitor. TX: Breast CA

(C in CMF), Hodgkins,

NH, leukemia

Mechlorethamine

Effect:


linking

Characteristics:

Derived from poison gas.

(The C in CMF). CausesImmunosuppression.


9/14

Cisplatin

Effect:


linking

Characteristics:

SIDE EFFECT = Renal

Insufficiency.

Doxorubicin/

Adriamycin

Effect:

Topoisomerase Inhibitor

Characteristics:

causes cardiotoxicity so

must limit LIFETIME dose

(women > men). TX:

Breast CA in AC combo

for those that not

respond to CMF TX

Irinotecan

Effect:

Topoisomerase Inhibitor

Characteristics:

TX: Colon CA with

FOLFIRI combo (FOL =

folinic acid - leucovorin,

F=5-FU, IRI = irinotecan)

5-FU

Effect:

Anti-Metabolite

Characteristics:

inhibits thymidylate

synthase needed for

dUMP to dTMP

competitively = no DNA

synthesis. TX: Breast CA

(F in CMF) and colon CA

(F in FOLFIRI). Increasedcytotoxicity via

metotrexate and

leukovorin


10/14

Methotrexate

Effect:

Anti-Metabolite

Characteristics:

Blocks DHFR = not make

dTMP = no DNA

synthesis. TX: Breast CA

(M in CMF). Side effects:

nephrotoxicity,

neurotoxicity, bone

marrow suppression

Leucovorin

Effect:

antidote to methotrexate

toxicity

Characteristics:

Used to rescue normal

cells in the bone marrow

from toxic effects of

methotrexate (in excess

also allows 5-FU to

inhibit more efficientyl)

Trastuzumab

Effect:

mAb - humanized

Characteristics:

Targets HER2 seen in

aggressive Breast CA

(poor prognosis), with

chemo = increase in

survival. Also causes

cardiac toxicity

Cetuximab

Effect:

mAb - chimeric

Characteristics:

targets EGFR inmetastatic colorectal CA.

When used with FOLFIRI

is only benefit if have

wild type Kras. Have GI

and skin side effects

(rash and

vomit/diarrhea)


11/14

Rituximab

Effect:

mAb - chimeric

Characteristics:

Destroys B cells and

tehrefore used to treat

disease characterized by

excessive numbers of B

cells. Tx: Lymphomas,

Leukemias, Transplant

rejection, autoimmune

disorders.

Bevacizumab

Effect:

mAb - humanized

Characteristics:

Neutralizes circulating

VEGF receptors which

prevents angiogenesis

but not work and causes

HTN. So only use is in

Macular Degeneration

Gefitinib

Effect:

Small Molecule Kinase

Inhibitor: EGFRCharacteristics:

Target: EGFR receptor.

Side effect = skin toxicity

(present in everyone)

Erlotinib

Effect:


Inhibitor: EGFR

Characteristics:

Target: EGFR receptor.Not work against

mutated T790 gene.


12/14

Lapatinib

Effect:


Inhibitor: HER2

Characteristics:

very selective for HER2 -

is most selective KI

Imatinib

(Gleevec)

Effect:


Inhibitor: Bcr/Abl

Characteristics:

targets the wild type abl

receptor in CML.

Resistance develops

quickly

Sorafenib

Effect:


Inhibitor: VEGFR

Characteristics:

Broad Spectrum inhibitor,

but primary target is

VEGFR

Sunitinib

Effect:

Small Molecule KinaseInhibitor: VEGFR

Characteristics:

Broad Spectrum inhibitor,

but primary target is

VEGFR


13/14

Bortezomib

Effect:


Inhibitor: Proteosome

inhibitor

Characteristics:

Inhibits protease by

binding proteosome

machinery (in all cells

though) causing CA cell

apoptosis. Used in

multiple Myeloma. Side

effects are many

including neutropenia

Vemurafenib

Effect:


Inhibitor: BRAF

Characteristics:

Specific inhibitor of

mutant BRAF in

Melanoma. A major side

effect is squamous cell

cancer in 12% of patients

Ipilimumab

Effect:

T-Cell Modulator:Blocking

Antibody increases T-cell

reaction

Characteristics:

Enhanced T-cell reaction

and more potent anti-

tumor reaction by

blocking CTLA-4(an

inhibitor receptor). Side

effects of rashes anddiarrhea/colitis


14/14

Anti-PD1

Effect:

T-Cell Modulator:Blocking

Antibody results in

preferential T-cell

activation

Characteristics:

Enhanced T-cell reaction

and more potent anti-

tumor reaction by

blocking interaction

between PD-1 and PD-L1

which signal T cells to

apoptose. Side effects of

rashes and

diarrhea/colitis

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