NAPLEX: Pharmacy Foundations - Basic Science Concepts

parasympathetic nervous system

rest and digest

Releases ACh → binds to muscarinic receptors → SLUDD (salivation, lacrimation, urination, defecation, digestion)

sympathetic nervous system

fight or flight

Releases Epi and NE → adrenergic receptors (A1, A2, B1) → ↑ BP, HR, bronchodilation → functions like digestion and urination minimized to focus on more important bodily functions for fight or flight

muscarinic receptor

- endogenous substrate

- agonist action

- drug agonists

endogenous substrate: ACh

agonist action: ↑ SLUDD

drug agonists

- Pilocarpine

- Bethanechol

muscarinic receptor

- endogenous substrate

- antaagonist action

- drug antagonists

endogenous substrate: ACh

antagonist action: ↓ SLUDD

drug agonists

- Atropine

- Oxybutynin

nicotinic receptor

- endogenous substrate

- agonist action

- drug agonists

endogenous substrate: ACh

agonist action: ↑ HR, BP

drug agonists

- Nicotine

nicotinic receptor

- endogenous substrate

- antagonist action

- drug antagonists

endogenous substrate: ACh

antagonist action: neuromuscular blockade

drug antagonists: neuromuscular blockers (ex: rocuronium)

alpha 1 receptor

- endogenous substrate

- agonist action

- drug agonists

endogenous substrate: epinephrine, norepinephrine

agonist action:

- smooth muscle vasoconstriction

- ↑ BP

drug agonists:

- phenylephrine

- dopamine (dose dependent - high dose)

alpha 1 receptor

- endogenous substrate

- antagonist action

- drug antagonists

endogenous substrate: epinephrine, norepinephrine

antagonist action:

- Smooth muscle vasodilation

- ↓ BP

drug antagonists: Alpha 1 blockers (doxazosin, carvedilol, phentolamine)

alpha 2 receptor

- endogenous substrate

- agonist action

- drug agonists

endogenous substrate: epinephrine, norepinephrine

agonist action

- ↓ release of epinephrine, norepinephrine

- ↓ BP, HR

drug agonists

- Clonidine

- Brimonidine

alpha 2 receptor

- endogenous substrate

- antagonist action

- drug antagonists

endogenous substrate: epinephrine, norepinephrine

antagonist action: ↑ BP, HR

drug antagonists:

- Ergot alkaloids

- Yohimbine

beta 1 receptor

- endogenous substrate

- agonist action

- drug agonists

endogenous substrate: epinephrine, norepinephrine

agonist action:

- ↑ myocardial contractility

- CO

- HR

drug agonists

- Dobutamine

- Isoproterenol

- Dopamine (dose dependent - medium dose)

beta 1 receptor

- endogenous substrate

- antagonist action

- drug antagonists

endogenous substrate: epinephrine, norepinephrine

antagonist action: ↓ CO, HR

drug antagonists: Beta 1 selective blockers (metoprolol) and non selective beta blockers (propranolol, carvedilol)

beta 2 receptor

- endogenous substrate

- agonist action

- drug agonists

endogenous substrate: epinephrine

agonist action: bronchodilation

drug agonists

- Albuterol

- Terbutaline

- Isoproterenol

beta 2 receptor

- endogenous substrate

- antagonist action

- drug antagonists

endogenous substrate: epinephrine

antagonist action: bronchoconstriction

drug antagonists: Non selective beta blockers (propranolol, carvedilol)

dopamine receptor

- endogenous substrate

- agonist action

- drug agonists

endogenous substrate: dopamine

agonist action: Many including renal, cardiac, and CNS effects

drug agonists:

- Levodopa

- Pramipexole

dopamine receptor

- endogenous substrate

- antagonist action

- drug antagonists

endogenous substrate: dopamine

antagonist action: Many, including renal, cardiac, and CNS effects

drug antagonists: 1st gen antipsychotics (haloperidol, metoclopramide)

serotonin receptor

- endogenous substrate

- agonist action

- drug agonists

endogenous substrate: serotonin

agonist action: Many including platelet, GI, and psychiatric effects

drug agonists: Triptans (sumatriptan)

serotonin receptor

- endogenous substrate

- antagonist action

- drug antagonists

endogenous substrate: serotonin

antagonist action: Many including platelet, GI, and psychiatric effects

drug antagonists: Ondansetron

2nd gen antipsychotics (quetiapine)

acetylcholinesterase

- endogenous effects

- drug action

endogenous effects: Breaks down acetylcholine

drug action (acetylcholinesterase inhibitors): Blocks acetylcholinesterase → ↑ ACh levels

angiotensin converting enzyme (ACE)

- endogenous effects

- drug action

endogenous effects: Converts angiotensin I → II (potent vasoconstrictor)

drug action: Inhibit production of angiotensin II → ↓ vasoconstriction + ↓ aldosterone secretion

catechol o methyltransferase (COMT)

- endogenous effects

- drug action

endogenous effects: Breaks down levodopa

drug action: Blocks COMT enzyme to prevent peripheral breakdown of levodopa → ↑ duration of action of levodopa

cyclooxygenase (COX)

- endogenous effects

- drug action

endogenous effects: Coverts arachidonic acid → PG (causes inflammation) and thromboxane A2 (causes platelet aggregation)

drug action: Block COX enzymes → ↓ PG and thromboxane A2

monoamine oxidase (MAO)

- endogenous effects

- drug action

endogenous effects: Breaks down catecholamines (DA, NE, Epi, 5-HT)

drug action: Block MAO which ↑ catecholamine levels

phosphodiesterase (PDE)

- endogenous effects

- drug action

endogenous effects: Breaks down cyclic guanosine monophosphate (cGMP) - a smooth muscle relaxant

drug action: Competitively binds to same active site as cGMP on PDE-5 enzyme → prevents breakdown of cGMP + prolonging smooth muscle relaxation

vitamin K epoxide reductase

- endogenous effects

- drug action

endogenous effects: Converts vitamin K to active form required for production of select clotting factors

drug action: Blocks vitamin K epoxide reductase enzyme which ↓ production fo clotting factors II, VII, IX, X

xanthine oxidase

- endogenous effects

- drug action

endogenous effects: Breaks down hypoxanthine into xanthine and xanthine into uric acid

drug action: Blocks xanthine oxidase enzyme → ↓ uric acid production

meds / foods that cause additive effects leading to hypertensive crisis

increased catecholamines

Bupropion

SNRI

TCA

Simulants

Levodopa

Linezolid

Methylene blue

Tyramine (from food)

meds / food that cause additive effects leading to serotonin syndrome

increased serotonin

SSRI

SNRI

TCA

Mirtazapine

Trazodone

Triptans

Opioids

Tramadol

Buspirone

Lithium

Dextromethorphan

St Johns Wort

drug structure contents

amoxicillin

Beta lactam ring fused to 5 sided ring

drug structure contents

ceftriaxone

Contains beta lactam ring fused to 6 sided ring

drug structure contents

ertapenem

Contains beta lactam ring fused to 5 sided ring

drug structure contents

aztreonam

Contains lactam ring NOT fused to another ring

drug structure contents

gentamicin

Contains amino group and sugar (glycoside) group

drug structure contents

sulfamethoxazole

Contains sulfonamide group

drug structure contents

aspirin

Contains an acidic, carboxyl group

drug structure contents

ibuprofen

Contains a carboxyl group

drug structure contents

amphetamine

Contains a primary amine functional group

drug structure contents

levothyroxine

Contains 4 iodine molecules in the structure

drug structure contents

amiodarone

Contains 2 iodine molecules in the structure

drug structure contents

fenofibrate

Contains ketone groups

drug structure contents

amitriptyline

Contains 3 rings in the structure

drug structure contents

chlorpromazine

Contains a thioether group

reactions that cause drug degradation

- oxidation reduction

- hydrolysis

- photolysis

oxidation reduction

- definitions

- sx

- prevention

loses electrons and is reduced when it gains electrons

sx: visible color change

prevention

- light protection

- temperature control

- antioxidants

- chelating agents pH control

hydrolysis

- definition

- prevention

water causes cleavage of a bond in a molecule

prevention: oxidation + protect from moisture

- light protection

- temperature control

- antioxidants

- chelating agents pH control

- adsorbents (dessicants)

- lyphilized powders - only reconstitute into solution shortly before use

- hygroscopic salt

photolysis

- prevention

protect from light