Test 1 Pharm: Module 1 & 6

Front 1

Hydrogen Bond

Back 1

Hydrogen atoms bound to nitrogen or oxygen become more positively polarized, allowing them to bond to more negatively polarized atoms such as oxygen, nitrogen or sulfur

2nd strongest bond

Front 2

Covalent Bonds

Back 2

Two bonding atoms share electrons

Strongest bond

Front 3

Ionic Bond

Back 3

Atoms with an excess of electrons (imparting an overall negative charge on the atom) are attracted to atoms with a deficiency of electrons (imparting an overall positive charge on the atom)

3rd strongest bond

Front 4

Van der Waals

Back 4

Shifting electron density in areas of a molecule, or in a molecule as a whole, results in the generation of transient positive or negative charges - these areas interact with transient areas of opposite charge on another molecules

Weakest bond

Front 5

Pharmacodynamics

Back 5

What the drug does to the body

Front 6

Pharmacokinetics

Back 6

what the body does to the drug (bioequivalence)

Front 7

Efficacy

Back 7

The Emax = maximal response produced by the drug

Front 8

Potency

Back 8

EC50 = the concentration at which the drug elicits 50% of its maximal response

Front 9

Hydrophilic

Back 9

*Water-loving/water-soluble
*Polar, usually ionized
*Renal excretion
*Requires transport mechanism to cross cell membranes & BBB
*Forms H+ bonds

Front 10

Hydrophobic

Back 10

*Lipophilic
*Fat-loving/water insoluble
*Passively diffuses across cell membranes and BBB
* Non-polar, usually not ionized

Front 11

Full Agonists

Back 11

*Maximum response/cellular effect
*Causes maximal change in cellular activity of target
*Stabilizes DR*

Front 12

Partial Agonist

Back 12

*Partial response
*Activates receptor without maximal efficacy
*Stabilizes DR and DR*

Front 13

Inverse Agonist

Back 13

*Inactivates free active receptors
*Stabilizes DR in the case of R*

Front 14

Competitive Antagonists

Back 14

*Reduces potency but not efficacy
*Reversible binding blocks agonist at active site
* Stabilizes DR, prevents DR*

Front 15

Noncompetitive Antagonists

Back 15

*Irreversible binding blocks agonist at active or allosteric site
*Reduces efficacy
* Stabilizes DR, prevents DR*

Front 16

ED50

Therapeutic Effect

Back 16

50% patients have therapeutic effect

Front 17

TD50

Toxic Dose

Back 17

50% have toxicity (side effects)

Front 18

LD50

Lethal Dose

Back 18

50% have lethal effects

Front 19

TI

Therapeutic Index

Back 19

TD50/ED50

High TI = good = optimal
Low TI = small window = hard to manage

Front 20

pKa

Back 20

pH at which 50% of the drug is ionized

Front 21

Pharmacokinetics: Absorption

Back 21

GI Tract/Parenteral/Skin/Membranes

How quickly can it leave GI tract
Bioavailability reaches & how much gets

Front 22

Pharmacokinetics: Distribution

Back 22

Blood/Target Tissue

Vd effected: drugs with a low volume of distribution may be highly protein bound

Front 23

Pharmacokinetics: Metabolism

Back 23

Liver/Tissue/Blood/CYP450 enzymes

Affected by substrate, inhibitor, inducer

Front 24

Pharmacokinetics: Excretion/Elimination

Back 24

Kidney/lungs/fecal

Front 25

Low Vd

Back 25

Retained in Vascular compartment

Front 26

High Vd

Back 26

Highly distributed into non-vascular compartments

Front 27

Vd

Back 27

= Dose/[drug] plasma

volume of fluid required to contain the total amount of drug absorbed in the body at uniform concentrations equal to that in the plasma steady state

Front 28

Pharmacokinetics

Back 28

True:
*Nonionized, lipophilic drugs favored for oral absorption
*Weak acids are best absorbed in the stomach
*Weak bases are best absorbed by the small intestine

Front 29

Protein Binding

Back 29

*Drugs must be free (non-protein bound) in order to reach its site of action and be metabolized and eliminated
*Drugs with a LOW Vd may be highly protein bound and more likely to remain in the plasma compartment

Front 30

Metabolism: Phase 1

CYP450 Induction

Back 30

Increase transcription with translation
Decrease degradation
Induction by another drug or autoinduction

Front 31

Metabolism: Phase 1

CYP450 Inhibition

Back 31

Incidental or deliberate
Competitive inhibition
Irreversible inhibition

Front 32

Drug Toxcities

Back 32

Intended Tissue - have an intended receptor ("On-Target" adverse effects) and an unintended receptor ("Off-Target" adverse effects)

Unintended Tissue - also have an intended receptor ("On-Target" adverse effects) and an unintended receptor ("Off-Target" adverse effects)

Front 33

Primary Neurotransmitter in the SNS is...

Back 33

Norepinephrine

Front 34

Primary Neurotransmitter in the PNS

Back 34

Acetylcholine

Front 35

Sympathetic Neurotransmitters

Back 35

Preganglionic - Ach & Nicotinic Receptor

Postganglionic - Ach or NE

Tissue Receptor - Muscarinic

Front 36

Parasympathetic Neurotransmitters

Back 36

Preganglionic - Ach & Nicotinic Receptor

Postganglionic - Ach

Tissue Receptor - Muscarinic

Front 37

Somatic Neurotransmitter

Back 37

Ganglionic - Ach

Tissue Receptor - Nicotinic

Front 38

Catecholamines

Back 38

Dopamine, Norephinephrine, Epinephrine

All synathesized from Tyrosine

Adrenergic receptors regulates release
Post synaptic adrenergic receptors are also effected

Front 39

Ephinephrine

Back 39

Nonselective Sympathomimetic Drug

Direct Acting

a1=a2; B1=B2

Front 40

Norepinephrine

Back 40

Nonselective Sympathomimetic Drug

Direct Acting

a1=a2; B1>>B2

Front 41

Isoproterenol

Back 41

Nonselective Sympathomimetic Drug

Direct Acting

B1

Front 42

Dopamine

Back 42

Nonselective Sympathomimetic Drug

Direct Acting

D1/D2, B1, a1

causes renal vasodilation at low doses and cardiac stimulation and vasoconstriction at high doses

Front 43

Amphetamine, methamphetamine, methylphenidate

Back 43

Nonselective Sympathomimetic Drug

Indirect Acting

Enhance release of catecholamines

Front 44

MAO-A

Back 44

inhibits breakdown of NE and EPI, allowing for shorter duration of action in the synapses

Front 45

Alpha-1 Agonist

Back 45

Increase PVR and BP
Mydriasis
Decongestant Activity

Front 46

Alpha-1 Antagonist

Back 46

Lower PVR and BP
Muscle relaxation in prostate and bladder

Front 47

Alpha-2 Agonists

Back 47

Lower PVR and BP
Decrease sympathetic outflow and BP
Reduce intraocular pressure

Front 48

Alpha-2 Antagonists

Back 48

Increase PVR and BP
Increase NE release from nerve terminals

Front 49

B1-agonism

Back 49

Increase force and rate of heart contraction

Front 50

B2-agonism

Back 50

Smooth muscle relaxation - respiratory, vascular, uterine

Front 51

B-antagonism

Back 51

Decrease production of aqueous humor
Bronchoconstriction
Decreased HR, contractility and BP

Front 52

DA-agonism

Back 52

Renal vasodilation, modulates NT release

Front 53

DA-antagonism

Back 53

Atypical antipsychotics

Front 54

Non-Selective Adrenoreceptor Agonists

Back 54

Norepinephrine and Epinephrine

Front 55

AChE inhibitors

Back 55

Increase levels of Ach
Use: myasthenia gravis, glaucoma, Alzheimers

Front 56

Nicotinic Agonists and Antagonists

Back 56

Agonists - continuous activation (depletion)
Antagonists - Ach blocked from binding

Use: neuromuscular paralyzing agent

Front 57

Muscarinic agonists

Back 57

Use: diagnosis of asthma, GI/GU motility, decrease intraocular pressure

Front 58

Muscarinic antagonists

Back 58

Use: Motion sickness, brochodilator, overactive bladder, bradycardia, mydriasis

Front 59

Muscarinic Effects

Back 59

"SLUG BAM", "SLUDGE"
*Salivation, Secretions, Sweating *S/S/S
*Lacrimation *Lacrimation
*Urination *Urination
*GI Upset *Diarrhea
*Bradycardia/bronchoconstriction/ *GI Upset
BM *Emesis
*Abdominal Cramps/Anorexia
*Miosis

Front 60

Anticholinergic Effects

Back 60

"ABCDS", "Can'ts"

*Anorexia *Can't PEE
*Blurry Vision *Can't SEE
*Constipation/Confusion *Can't SPIT
*Dry Mouth *Can't SH$T
*Sedation/Stasis of Urine