Equation for

half-life, volume of distribution & clearance

 T _1/2 = (0.7 * V_D ) / CL

Equation for Clearance

Rate of elimination of drug / Plasma drug concentration

V_D (volume of distribution) * K_e (elemination constant)

Equation for Loading Dose

[Drug]_plasma * V_D / Bioavailaility

Equation for Maintenance Dose

[Drug]_plasma * Clearance / Bioavailability 

Zero Order Eliminated Drugs

"PEA"

Phenytoin

Ethanol

Aspirin (at toxic doses)

Capacity-limited elimination

Therapeutic Index

Drug Safety Measurement

"TILE"

Therapeutic Index = LD₅₀/ED₅₀

Drugs with Low Therapeutic Index

 "Toxic side effects come easy 

With These Little Drugs"

Warfarin

Theophylline

Lithium

Digoxin

 GCPR's

 Mnemonic for G_q coupled receptors

"HAVe 1 M&M"

 H1, α1, V1

M1 & M3

GPCRs

Mnemonic for G_i coupled receptors

"MAD 2's"

M2

α2

D2

GPCRs

Mnemonic for G_i/s/q of all receptors

"qiss & qiq till

you're siq of sqs (super qinky sex)"

α1 = q, α2 = i, β1 = s, β2 = s

M1 = q, M2 = i, M2 = q

D1 = s, D2 = i

H1 = q, H2 = s

V1 = q, V2 = s

α1 receptor

functions

1. Vasoconstriction
2. Myadriasis (pupillary dilation)
3. Intestinal/Bladder Retention (sphincter)

α2 receptor

functions

1. ↓SNS outflow
2. ↓Insulin release
3. ↓Lypolysis
4. ↑Platelet  aggregation

β1 receptor

functions

1. Heart - ↑HR, ↑contractility
2. Kidneys - ↑Renin
3. ↑Lipolysis

β2 receptor

functions

1. Vasodilation, Bronchodilation
2. Heart - ↑HR, ↑contractility
3. ↑Insulin release, ↑Lipolysis
4. ↓Uterine tone (tocolysis)
5. Far-vision accomodation (ciliary m. relaxation)
6. Aqueous humor production

M1 receptor

functions

1. CNS
2. Enteric nervous system

M2 receptor

functions

Heart - ↓HR, ↓atrial contractility

M3 receptor

function

D1 receptor

functions

Renal vasodilation

D2 receptor

functions

CNS - NT release modulation 

H1 receptor

functions

1. Mucus production - nasal, bronchial
2. Bronchoconstriction
3. Pruritus
4. Pain

H2 receptor

function

V1 (ADH) receptor

function

Vasoconstriction

V2 receptor

function

H2O reasortion in CT

Hemicholinium

Presynaptic ACh Inhibitor

Choline reuptake inhibitor

Vesamicol

Presynaptic ACh Inhibitor

=Acetyl Choline Transferase Inhibitor

(Vesicular Transporter)

Botulinum toxin

(Botox)

 Presynaptic ACh Inibitor

 Inhibits ACh release

Metyrosine

 Presynaptic NE Inhibitor

Tyrosine hydroxylase inhibitor

(Tyrosine → DOPA)

Reserpine

 Presynaptic NE Inhibitor

Vesicular monoamine transporter inhbitor

(Vesicular loading)

(Dopamine → NE)

Guanethidine & Bretyllium

 Presynaptic NE Inhibitors

Inhibit NE release

Presynaptic SNS

Release-modulating Receptors

M2 & α2 → ↓NE release

Angiotensin II R→ ↑NE release

Bethanechol

mAChR agonist

"Bethany call me, maybe, if you wanna activate your baldder & bowels"

Post-Op/Neurogenic ileus

Urinary retention

Carbachol

mAChR agonist

"Carbon copy of achetylcholine"

Glaucoma

Pupil constriction

Relief of intraocular pressure

Pilocarpine

mAChR agonist

"Cry, drool & sweat on your pillow"

↑Sweat, tears, saliva (Sjogren's)

Open-angle glaucoma (ciliary m. contraction)

Closed-angle glaucoma (pupil constriction)

Resistant to AChE

Methacholine

mAChR agonist

Challenge test for asthma diagnosis

(bronchoconstriction w/inhalation)

Neostigmine

PNS AChE inhibitor

"Neo = No CNS penetration"

Post-op & neurogenic ileus

Urinary retention

Myasthenia Gravis

Post-op NMJ blockade reversal

Pyridostigmine

PNS AChE inhibitor

P = PNS only (No CNS)

Pyridostrigmine gets rid of myasthenia gravis

 Myasthenia gravis (long-acting)

↑Strength

Edrophonium

AChE inhibitor

Myasthenia gravis Diagnosis

(extremely short-acting)

Physostigmine

AChE inhibitor

"Physostigmine phyxes atropine OD"

Anti-cholinergic toixicity

Crosses the BBB → CNS

Donepezil

AChE inhibitor

"Give old man Don his memory pezil"

Alzheimer's drug

AChE inhibitors

Cautionary-Use Conditions

COPD

Asthma

PUD

Organophosphate

(parathion, insecticide)

Toxidrome

Irreversible AChE inhibitors

"DUMBBELSS"

Diarrhea, Urination, Miosis

Bronchospasm, Bradycardia, 

Excitation muscles/CNS, Lacrimation

Sweating, Salivation

 Often seen in farmers

Organophosphate

(Parathion, insecticide)

Antidote

Atropine

(anti-muscarinic)

+

Pralidoxime 

(regenerates active AChE)

Atropine

Homatropine

Tropicamide

mAChR antagonists

EYES

Mydriasis

Cycloplegia (lack of accomodation)

Benztropine

CNS mAChR antagonist

"Park my Benz"

 Parkinson's disease

improves tremor & rigidity, NO effect on bradykinesia

Anti-psychotic side effects

Scopolamine

CNS mAChR antagonist

"Scoping out our ship's horizons"

Motion sickness

Ipratropium

Tiotropoim

mAChR antagonist

LUNGS

"I pray I an breathe soon"

COPD & Asthma

Ipra = short-acting

Tio = long-acting

Oxybutynin

mAChR antagonist

GU

↓Urinary urgency (mild cystitis)

↓Bladder spasm

Glycopyrrolate

mAChR antagonist

GI & LUNGS

Parenteral: pre-op =↓airway secretion

post-op = NMJ block reversal (w/neostigmine)

Oral: drooling, PUD

Atropine

mAChR antagonist

Bradycardia

Ophthalmic (mydriasis, cycloplegia)

Anti-Cholinergic

(Atropine)

Toxidrome

HOT as a hare - fever (infants)

DRY as a bone - ↓sweating, dry mouth

RED as a beet - flushed skin

BLIND as a bat- cycloplegia, myadriasis

(acute angle-closure glacoma - elderly)

MAD as a hatter - disorientaed

FAST as a cheetah - ↑HR

FULL as a tick - urinary retention (BPH)

QUIET as a mouse - absent bowel sounds/constipation

Jimson Weed (Datura)

Anti-muscarinic

"Gardner's pupil" - Myadriasis

Bella donna plant alkaloid

Epinephrine

Receptor Activity & Uses

β1 & β2 > α1 & α2

Anaphylaxis, Hypotention

Open-angle glaucoma

Asthma

Norepinephrine

Receptor Activity & Uses

α1 & α2 > β1  (NOT β2)

Hypotention but ↓renal perfusion

Isoproterenol

β1 & β2 agonist

Torsades de pointes

Bradycardic arrythmias

(but can worsen ischemia)

Dopamine

Receptor activity & Uses

Low dose -  D1

Medium dose - β1,  β2

High dose - α1, α2

Shock w/ renal perfusion

Heart failure - Ionotropic & Chronotopic

Dobutamine

Receptor activity & Uses

β1 >> α1, α2, β2

Heart failure - ionotropic & chronotropic

Cardiac stress testing

Phenylephrine

Receptor activity & Uses

α1 > α2

Hypotention (vasoconstriction)

Ocular procedures (mydriasis)

Rhinitis (decongestant)

Albuterol

Metaproterenol

Short-acting β2 agonists

(Some β1 activity)

Acute asthma (rescue inhalers)

Salmeterol

Formoterol

Long-acting β2 agonists

(Some β1 activity)

Long-term asthma (control inhalers)

Terbutaline

β2 agonist

(Some β1 activity)

"Stop a turbulent uterus"

 Reduce premature contractions

Ritodrine

Selective β2 agonist

"Right her drain"

↓Premature contractions

Amphetamine

MOA & Uses

Indirect sympathomimetic

(↑presynaptic catecholamine release)

Narcolepsy, obesity, ADHD

Ephedrine

MOA & Uses

Indirect sympathomimetic

(↑presynaptic catecholamine release)

Nasal decongestant

Urinary incontinence

Hypotention

Cocaine

MOA & Consequences

Indirect sympathomimetic

(Catecholamine Reuptake inhibitor)

Vasoconstriction, Local anesthetic

 Never give β-blockers in Cocaine intoxication

→unapposed α1 activation & extreme HTN

Norepinpehrine

vs.

Isoproterenol

NE (α>β) = ↑BP + reflex bradycardia

Isoproterenol (β>α) = ↓BP + tachycardia

Clonidine

α-methyldopa

α2 agonists

↓SNS outflow

Hypotension esp. w/renal disease

(no ↓renal perfusion)

Phenoxybenzamine

Non-selective irreversible

α antagonist

Pheochromocytoma

(esp. before tumor removal)

Phentolamine

Nonselective, Reversible

α antagonists

MOA-inhibitor patients

who eat tyramine-containing products

Prazosin

Terazosin

Doxazosin

Tamsulosin

Selective

 α1 antagonists

Hypertention

Urinary retention in BPH

Mirtazapine

Selective α2 antagonist

Depression

Adverse H1 effects = sedation, ↑cholesterol, ↑appetite

Selective β1 Blockers

"A BEAM to the heart"

Acebutolol (partial)

Betaxolol

Esmolol (short-acting)

Atenolol

Metoprolol

Nonselective β-blockers

"Please Try Not βeing Picky"

Propranolol

Timolol

Nadolol

β-blockers (β1=β2)

Pindolol

Nonselective β-blockers

w/ α1 antagonist activity

"The -olol's without an 'o'"

Carvedilol

Labetalol

Vasodilators

β-blocker

Adverse Effects

1. Impotence (↓vasodilation)
2. Asthma exacerbation (↓bronchodilaiton)
3. CV - bradycardia, AV block, CHF
4. CNS - seizures, sedation, sleep alt.
5. ↓Insulin release - caution in diabetics

β-blocker

Uses

Angina - ↓O2 consumption by heart
Post-MI - ↓Mortality 
SVT (metoprolol, esmolol) - Class II anti-arrythmics, ↓AV conduction velocity
HTN - ↓CO, ↓renin
CHF - slows progression
Glaucoma (timolol) - ↓aqueous humor production

Cardioprotective β-Blockers

"Make my Cardio Beat"

Metoprolol

Carvedilol

Bisprolol

Activate β-arrestin pathway

Partial β-agonists

"PAPA"

Pindolol

Acebutalol

Acetaminophen

Antidote

N-acetylcysteine

(↑glutathione)

Salicylates

Antidote

NaHCO3  (alkalinize urine)

Dialysis

Amphetamine / Local Anesthetic (base)

Antidote

NH4Cl (acidify urine)

AChE inhibitor / Organophosphate

Antidote

Atropine + Pralidoxime

Anti-Muscarinic / Anti-Cholinergic

Antidote

Physostigmine

&

Control hyperthermia

β-Blocker

Antidote

Glucagon

Digitalis

Antidose

"KLAM"

K+

Lidocaine

Anti-Dg Fab fragment

Mg2+

Iron

Antidote

Deferoxamine

Deferasirox

Lead

Antidote

Ca-EDTA

Dimercaprol

Succimer

Penicillamine

Iron, Mercury, Arsenic, Gold

Antidote

Dimercaprol (BAL)

Succimer

Iron, Copper, Arsenic Gold

Antidote

Penicilliamine

Cyanide

Antidote

Nitrite + thiosulfate

Hydroxocobalamin

Methemoglobin

Antidote

Methylene blue

Vitamin C

Carbon monoxide

Antidote

100% O2

Byperbaric O2

Methanol

Ethylene glycol (anti-freeze)

Antidote

Fomepizole > Ethanol

Dialysis

Opioid

Antidote

Nalozone (short-acting)

Naltrezone (long-acting)

Benzodiazepine

Antidote

Flumazenil

TCA

Antidote

NaHCO2

(plasma alkalinization)

Heparin

Antidote

Protamine

Warfarin

Antidote

Vitamine K 

Fresh frozen plasma (acute)

tPA, streptokinase, urokinase

Antidote

Aminocaproic acid

Theophylline

Antidote

β-blocker

Adverse effect:

Coronary vasospasm

Cocaine

Sumatriptan (migraine prophylaxis)

Ergot alkaloids (DA agonists)

Adverse effect:

"VANC"

Vancomycin - Red Man syndrome

Adenosine

Niacine

Ca2+ channel blockers

Adverse effect:

Doxorubicin (Adriamycin)

Daunorubicin

Adverse effect:

Anti-Arrhythmics:

Class III - sotalol

Class IA - quinidine

Adverse effect:

"Agranulocytosis Could Certainly Cause Pretty Major Damage"

Clozapine, Carbamazepine, Colchicine

Propylthiouracil, Methimazole

Dapsone

Adverse effect:

Chloramphenicol

Benzene

NSAIDs

Propylthiouracil, Methimazole

Adverse effect:

Direct Coombs-positive

Hemoytic Anemia

Methyldopa

Penicillin

Adverse effect:

Chloramphenicol

Adverse effect:

"Hemolysis IS PAIN"

Isoniazid

Sulfonamides

Primaquine

Aspirin

Ibuprofen

Nitrofurantoin

Adverse effect:

"Having a BLAST with PMS"

Phenytoin

Methotrexate

Sulfa drugs

Adverse effect:

OCPs

Adverse effect:

ACE inhibitors (bradykinin effect)

(ARBs like losartan = no cough)

Adverse effect:

It's hard to BLAB when you have pulmonary fibrosis

Bleomycin

Amiodarone

Busulfan

Acute Cholestatic Hepatitis

(Jaundice)

Erythromycin

Focal-Massive Hepatic Necrosis

Liver "HAVAc"

Halothane

Amanita phalloides 

Valproic acid

Acetaminophen

Adverse effect:

Hepatitis

Isoniazid

Adverse effect:

Clindamycin

Ampicillin

Adverse effect:

Glucocorticoid withdrawal

(HPA suppression)

Adverse effect:

Some Drug Creat Awkward Knockers

Spironolactone

Digitalis

Cimetidine

Alcohol (chronic use)

Ketoconazole

Estrogen

Adverse effect:

SERMs

Tamoxifen 

Clomiphene

Adverse effect:

Niacin

Tacrolimus

Protease inhibitors

HCTZ

Corticosteroids

Adverse effect:

Hypothyroidism

Lithium

Amiodarone

Sulfonamides

Adverse effect:

Glucocorticoids

Protease inhibitors

Adverse effect:

Phenytoin

Verapamil

Adverse effect:

Furosemide

Thiazides

Niacin 

Cyclosporin

Side Effects:

Myopathies

Fish N CHIPS Give you myopathies

 Fibrates, Niacine

Colchicine

Hydroxychloroquine

INFα

Penacillamine

Statins

Glucocorticoids

Side Effects:

Osteoporosis

Corticosteroids

Heparin

Side Effects:

Photosensitivities

SAT for a photo

Sulfonamides

Amiodarone

Tetracycline 

Side Effects:

Steven-Johnson Syndrome

Bad rash after a PEC SLAPP

Penicillin

Ethosuximide, Carbamazepine

Sulfa drugs

Lamotrigine

Allopurinol

Phenytoin, Phenobarbital