General Pharm And Autonomics

Front 1

Drugs to Avoid in Pregnancy

SAFE Moms Take Really Good Care

Back 1

Sulfonamides (kernicterus), Aminoglycosides (ototoxic), Fluoroquinilones (cartilage damage), Erythromycin (acute cholestatic hepatitis), Metronidazole (mutagenic), Tetracycline (discolored teeth), Ribavarin, Griseofulvin, Chloramphenicol (gray baby)

Front 2

Volume of Distribution

Back 2

Vd= amount of drug in body / plasma drug concentration

If bound to plasma proteins, this is altered in liver disease

Front 3

Clearance

Back 3

CL= rate of elimination / plasma concentration

Front 4

Half Life

Back 4

t1/2= [0.7 * Vd] / CL

If infused at a constant rate, it reached 94% of steady state in 4 t1/2

Front 5

Dosage Calculation

Back 5

Loading Dose = Desired Conc * [Vd/bioavailability]

Maintainance Dose= Desired Conc * [Clearance/Bioavailability]

In pts with Renal/Liver disease, the loading dose is constant, it's the maintainance dose that decreases

Front 6

Zero Order Elimination

Back 6

Cp (plasma conc) falls at a steady rate no matter what the starting point (linear decrease)

Ex- EtOH, Phenytoin, Aspirin

Front 7

First Order Elimination

Back 7

Rate of elimination is proportional to concentration (faster at high concentration, slower at low) -- exponential curve

Front 8

Excretion occurs in 2 phases

Phase 1 occurs in ____ and yields _____. An example is the ______ system

Phase 2 uses ______ and yields _______

Back 8

Liver
Oxidized and Reduced compounds that are slightly polar and still active
Cyt p450 System

Acetylation, Glucuronidation
Very polar substances that are inactive

Front 9

Competitive Antagonist

Will shift the curve to the _____

Back 9

To achieve the same % maximum effect req's a higher dose --> curve shifts to the right

Still able to achieve 100% max effect

Front 10

Irreversible Antagonist

Will shift the curve ______

Back 10

Decreases the % maximum effect --> shifts the curve downward.

Even at high concentrations of the drug, it cannot overcome the antagonist and it's effect is decreased

Front 11

EC(50) vs Kd

Back 11

Kd= dose req'd to occupy 50% of all receptors

EC(50)= dose req'd to get 50% of maximum effect --> this is most imp't clinically

EC(50) < Kd means that there are "spare receptors" or less than 50% receptors need to be occupied for activity

Front 12

Potency

Back 12

Dose req'd to get an effect...it is independent of full or partial agonist

Front 13

Full agonist v Partial Agonist

Back 13

Partial Agonist is never able to reach the same maximum effect as a Full Agonist (it has lower efficacy). However, the partial agonist can be more potent.

Front 14

Therapeutic Index

Back 14

TD50/ED50

Dose to get 50% people sick/ Dose to get 50% people better

Narrow Index= lower dose causes more toxic effects compared to therapeutic

Large Index(desirable)= need a higher dose to cause toxicity compared to effective dose

Front 15

Guanylate Cyclase q receptor

Back 15

HAV 1 M&M
H1, alpha 1, V1, M1, and M3

Front 16

Guanylate Cyclase i receptor

Back 16

MAD 2's
M2, alpha 2, D2

Front 17

Guanylate Cyclase s receptor

Back 17

B1, B2, D1, H2, V2

Front 18

Cholinomimetics (Direct Agonists)
1)Bethanechol
2)Pilocarpine

Back 18

1) Used for post-op ileus and bladder retention (Bowel and Bladder)

2)Used for Glaucoma by opening the angle via cilary muscle contraction and by dilating the pupilary sphincter. Works on narrow angle and open angle

Front 19

Cholinomimetics (Indirect via AChE inhibition)
1)Neostigmine
2)Pyridostigmine
3)Edrophonium
4)Physostigmine
5)Echothiophate

Back 19

1) Myasthenia gravis, post-op reversal of neuromuscular blockade

2)Myasthenia gravis

3)Short acting, used to diagnose Myasthenia gravis

4) Glaucoma -->able to cross BBB and Atropine overdose

5)Glaucoma

Front 20

Signs of Cholinesterase Poisoning

DUMBBELSS

Caused by Parathion and Organophosphates

Back 20

Diarhhea, Urination ,Miosis, Bronchospasm, Bradycardia, Excitation of muscles, Lacrimation, Sweat, Salivate

Trt- Atropine (blocks muscarinic receptors) and pralidoxime (regenerates AChE)

Front 21

Cholinoreceptor Blockers

1)Atropine,Homatropine
2)Benztropine
3)Ipatropium

Back 21

1) Used in eye to cause Mydriasis (dilation) and cycloplegia(can't focus)

2)Used in CNS for Parkinson's (blocks indirect pathway)
3) Used in Lungs for Asthma/COPD

Front 22

Atropine

Back 22

MOA= muscarinic anatogonist

Blocks Salivation, Lacrimation, Urination, and Defecation

Toxic= Hot, Dry, Red Flushed Skin, Vision problems, Disorientation

Front 23

Hexamethonium

Back 23

MOA= Blocks nicotinic receptors

Use= used to block vasovagal response to prevent reflex bradycardia with NE increase BP

Front 24

Epinephrine
1)receptor specificity
2)Low Dose
3)High Dose
4)Uses

Back 24

1) Beta>Alpha but more Alpha receptors in body
2) Binds only Beta receptors causing inc HR,Contractility via B1, but also Vasodilation via B2 --> no change in Blood Pressure
3) Mostly alpha receptor effects--> vasoconstriction causing increased BP....prevented by giving Alpha Blocker previously leading to decreased BP (Epi reversal)

4) Anaphylaxis, open angle glaucoma, asthma (B2 stim), hypotension

Front 25

NorEpi
1)receptors
2)Effects
3)Pretreat with Alpha blocker
4)Uses

Back 25

1) Alpha1 > Beta 1
2) causes increased vasoconstriction along with increased contractility leading to massive increase in BP --> reflex bradycardia
3)Will prevent pressor effect but no reversal to depressor like Epi
4) Hypotension

Front 26

Isoproterenol
1)receptors
2)effects

Back 26

1) only B1 and B2
2) decreases BP via B2 leading to reflex Tachy

Front 27

Dopamine
1)Receptors
2)Effects
3)Use

Back 27

1) D1=D2>Beta>Alpha
2)Low Dose= Renal vasodilation to help in cardiac shock
Med Dose= increase HR
High Dose= Increase Vasoconstriction to Inc BP
3) Cardiac Shock, Heart Failure

Front 28

Ephedrine
1)MOA
2)Use

Back 28

1)increase release of stored catecholamines
2)nasal decongestion, urinary incontinence, hypotension

Front 29

Phenylephrine
1)MOA
2)Uses

Back 29

1)Acts on Alpha receptors
2)Dilates pupil, vasoconstrictor, nasal decongestion

Front 30

Albuterol

Back 30

B2 agonist used in Asthma

Front 31

Clonidine and Methyldopa
1)MOA
2)Use

Back 31

1)Binds alpha 2 receptors in CNS to prevent catecholamine outflow
2) Hypertension in pts with renal disease because it won't decrease renal blood flow

Front 32

Nonselective Alpha Blockers

1) Irreversible is ____
2) Reversible is ______
3) Used to trt
4) Toxicity

Back 32

1)Phenoxybenzamine
2)Phentolamine
3)Pheochromocytoma
4)Hypotension with reflex tachy

Front 33

Alpha 1 blockers
Prazosin, Terazosin

Back 33

1) used in hypertension, urinary retention from BPH

2)can cause 1st dose hypotension and dizziness

Front 34

Beta Blockers

Back 34

All that start with A-->M are selective for B1 receptor (safe in asthmatics)

Used to lower BP, lower HR, slow CHF progression, lower Aqueous humor production (Glaucoma)

Toxicity- Impotence, Bradycardia, sedation, can cause hyperglycemia in Diabetics