Pharmacology

Question 1

Cholinesterase inhibitors

Answer 1

prolong ACh, which acts on the parasympathetic nervous system –> can be used a poison (shortest acting - alcohols, longest acting, organophosphates *aging)

Question 2

Nicotine

Answer 2

nAch receptors tend to desensitize at neuromuscular junction

Question 3

Muscarine

Answer 3

Mimics function of ACh in muscarinic part of cholinergic NS

Question 4

Atropine

Answer 4

Competetive muscarinic ACh antagonist –> block binding sites for ACh “dry as a bone, blind as a bat, red as a beet, mad as a hatter”

Question 5

Scopolamine

Answer 5

Muscarinic cholinergic antagonist (blocks PS) dilated eyes

Question 6

Neostigmine

Answer 6

Interferes with breakdown of ACh, stimulates muscarinic and nicotinic

Question 7

Pralidoxime

Answer 7

Antidote to AChE inhibitors, antagonize mAChR receptors and inhibit esterase inhibtor (cannot reach CNS) “chemical crowbar” with short time window due to aging

Question 8

Amphetamine

Answer 8

Indirect agonists: increase transmitter in synapse by promoting release

Question 9

Phenylephrine

Answer 9

Adrenergic agonist Alpha1 - increase peripheral arterial resistance and decrease venous capacitance, nasal decongestant

Question 10

Pseudoephedrine

Answer 10

Adrenergic - indirect agonist, presynaptic NE releasing agent, nasal decongestant

Question 11

Cocaine

Answer 11

NE reuptake blocker

Question 12

Clonidine

Answer 12

Adrenergic agonist Alpha2 - antihypertensive

Question 13

Prazosin

Answer 13

Alpha1 antagonist: hypertension

Question 14

Propranolol

Answer 14

prototype Beta1/2 blocker: hypertension, angina, arrythmias, migraine, anxiety

Question 15

Tyramine

Answer 15

Tyramine (wine, cheese, chocolate) leads to NA release, increase in BP

Question 16

Parasympathetic system

Answer 16

Organs of head, neck, trunk & external genitalia;

Cardiac and smooth muscle; gland cells; nerve terminals ACh Muscarinic

Question 17

Sympathetic

Answer 17

Organs of head, neck, trunk & external genitalia, sweat glands, adrenal medulla, arrector muscles of hair, all vascular smooth muscle
Sweat glands Muscarinic; cardiac and smooth muscle, gland cells, nerve terminal (all adrenergic - Alpha/Beta), renal vascular smooth muscle (dopamine)

Question 18

Catecholamine biosynthesis

Answer 18

Tyrosine –> DOPA –> Dopamine –> Norepinephrine –> Epinephrine

Question 19

Important Muscarinic receptors

Answer 19

M1 postganglionic neuron
M2 heart
M3 exocrine

Question 20

Difference between muscarinic and nicotinic receptors

Answer 20

M - g-protein coupled receptor, much slower than N which is a ligand gated ion channel

Question 21

Liver P450

Answer 21

Liver enzymes deactivate some drug molecules; P450 genetically determined, some lack CYP activities others have higher

Question 22

HPA Axis

Answer 22

Hypothalamus - sends neuropeptide (pituitary portal system) –> anterior pituitary - sends protein/peptide hormone (systemic circulation) –> Target organ

Question 23

Cortisol production

Answer 23

Paraventricular Nucleus (PVN) - sends Corticotropin releasing hormone –> Coriticotrope cell - sends ACTH (product of POMC, cleaved) –> Adrenal Cortex

Question 24

Where is cortisone produced in adrenal cortex?

Answer 24

Zone resticularis and fasiculata

Question 25

Pathway for ACTH?

Answer 25

Binds to a protein on the surface; causes reaction that activates P-StAR in mitochondria; stimulates cholesterol to produce steroid hormones

Question 26

Biocheical effects of glucocorticoids

Answer 26

• Maintain blood glucose
• Mobilize AAs
• Stimulate lipolysis in adipose tissues
• Catatonic/anabolic effects in bone
• Inhibit immune function/inflammation
  (glucocorticoid receptor is pretty much everywhere! What prevents it from having widespread effects in every organ is enzymes that can inactivate it, like in the kidney)

Question 27

Congenital Adrenal Hyperplasia

Answer 27

• Glucocorticoid insufficiency, increase in androgen production … pathway blocked so more sex hormone/androgen production

Question 28

Side effects of glucocorticoids

Answer 28

• Impaired glucose use
• Induction of diabetic state
• Osteoperosis
• Impaired wound healing
• Adrenal insufficiency
• Cushing’s syndrome

Question 29

Asthma drugs - target receptors

Answer 29

M3 antagonist or Beta2 agonist