Muscarinic receptors, nicotinic at high doses

metabolized by AChesterase

produces parasympathetic effects

Used in paralytic ileus and OAG

dangerous in asthmatics, hypothyroidism, GI obstruction

Muscarinic agonist, nicotinic at high doses

not metabolized by AChesterase

produces parasympathetic effects

used in OAG

Selective Muscarinic agonist

not metabolized by AChesterase

produces parasympathetic effects

Used in post-operative ileus and urinary retention

Selective Nicotinic agonist

Crosses the BBB

Produces excitation, addiction, increased arousal (amygdala, thalamus)

Stimulation of autonomic ganglia, increases GI tone

Used to aid in smoking cessation, ulcerative colitis, and Tourette's Syndrome

Side effects: nausea, vomiting

Associated with Mesolimbic reward system

Partial agonist at the Alpha4Beta1 nicotinic receptor

Activates nicotinic receptors somewhat less than nicotine

Blocks nicotines access to the receptor

Used in smoking cessation

Side effects: neuropsychiatric symptoms

Blocks AChesterase

Enhances the action of ACh at nicotinic receptors in high doses

Increases muscular contraction

Used as a myasthenia gravis diagnostic tool because it only lasts 5-15 minutes

Blocks AChesterase to enhance ACh

Causes constriction of ciliary muscle

Used in miotic glaucoma

30 min - 2 hour duration

Crosses the BBB

Blocks AChesterase to enhance ACh

Enhances action of ACh at nicotinic receptors at high doses

Used for myasthenia gravis (with atropine)

Used in gut/bladder atony or to reverse paralysis produced by skeletal muscle blockers

30 min - 2 hour duration

Blocks AChesterase

Modest improvements in memory and cognition

Used in Alzheimer's

24 hour duration

Crosses BBB

Available in pill or patch

Blocks AChesterase

Modest improvements in memory and cognition

Used in Alzheimer's

12 hour duration

Also enhances ACh binding to nicotinic receptors

Side effects: nausea, diarrhea, insomnia

Irreversibly binds AChesterase

Produces overstimulation of muscarinic receptors

SLUD

Side effects: bronchoconstriction, miosis, sweating, bradycardia, hypotension, pulmonary edema, respiratory paralysis, ataxia, confusion, convulsions, coma

Atropine will block muscarinic activation

Pralidoxime will reactive AChesterase

Blocks release of ACh into the synapse by cleaving SNAP25

Blocks effects of ACh at muscarinic receptors

Used for blepharospasm, cosmetic

Can cause excessive muscle paralysis

Blocks ACh activation of muscarinic receptors

Produces: tachycardia, prolonged mydriasis, inhibited secretions, constipation, retention, CNS excitement

No effect on blood vessesl

Used as a pre-anesthetic, anti-spasmodic, and anti-diarrheal

Crosses the BBB

Can be dangerous in OAG

Blocks ACh activation of muscarinic receptors

Bronchodilator

Used in COPD

Does not cross the BBB

Blocks every ganglionic nicotinic receptor in sympathetic and parasympathetic system. Thus is also blocks the adrenergic release of NE

Causes vasodilation, hypotension, tachycardia, mydriasis, reduced GI tone, decreased secretions, xerostomia, and decreased genital stimulation

Used in AAA and to rapidly control BP

Non-depolarizing skeletal nicotinic receptor blocker

Causes muscle paralysis

Used to eliminate muscle movements during surgery

Side effects: hypotension due to mast cell degranulation

Cam also block neuronal nicotinic receptors at high doses

2 hour duration

Does not cross BBB

Reversed by neostigmine + atropine

Non-depolarizing skeletal nicotinic receptor blocker

Causes muscle paralysis

Used in surgery

Side effects: less hypotension than tubocurarine

1 - 1.5 hour duration

Reversed by neostigmine + atropine

Depolarizing skeletal muscle nicotinic receptor blocker

Causes muscle paralysis

Used in endotracheal tube insertion

Lasts very short time

Metabolized by AChesterase

Cannot be reversed

Alternative: Rocuronium

Reactives ACh that has been blocked by irreversible anti-AChesterase

Reduces over-activation of muscarinic receptors

Sarin antidote

Skin, mucosa

Constriction of skeletal muscle BV

Constriction of ab viscera BV

Constriction of pulmonary BV

Contraction of GI sphincters

Contraction of bladder

Male and female orgasm and ejaculation

Uterine contraction in pregnant women

Epi > NE > Iso > DA > Doba

Increased HR, conduction, and contractility

Renin release from the JGA

Iso > Epi > NE > DA > Dobu

Dilation of skeletal muscle BV

Dilation of ab viscera BV

Decreased GI tone, increased motility, and secretion

Bladder relaxation

Uterine relaxation

Epi > NE > Iso > DA > Doba

Low dose: Beta 1 and Beta 2

High dose: Alpha 1

Beta 1: increased automaticity, rate, conduction, CO

Beta 2: decrease BP (low dose), bronchodilation, glycogen breakdown

Alpha 1: increase BP (high dose), bronchodilation, decreased glycogen synthesis, and decreased insulin secretion

Used in anaphylactic shock, hypersensitivity reaction, cardiac arrest

Neurotransmitter in postganglionic sympathetic neurons

Same effects on heart as epi

Increased BP (Alpha 1) with no change in cardiac output

Used in cases of shock and spinal anesthesia

Non-endogenous selective Beta agonist

Beta 1: Increase HR, etc

Beta 2: Decrease BP (vasodilation), bronchodilation

Used in emergent heart block, in preparation for a pacemaker, or to relax bronchi if Beta 2 selective agonist is not available

Will not cross BBB

Dopamine receptor, Beta 1, and Beta 2

High dose: Alpha 1

Beta 1: increases HR

BP net decreases due to above receptors

Used in cardiogenic shock

Side effects: excessive sympathetic stimulation and excessive dopamine stimulation (CTZ)

No CNS effects

Low dose: Beta 1

High dose: Beta 2, Alpha 1

Beta 1: Increase in HR but not contractility

Alpha 1: Increase in BP at high doses

Used in heart failure, open heart surgery, or acute MI

Side effects: Arrhythmias

A sympathomimetic

Does not cross BBB

An alpha agonist primarily selective for Alpha 1

Decongestion of mucous membranes and pupillary dilation

Side effects: excessive stimulation can elevate BP

Not metabolized by MAO or COMT

A weak Alpha and Beta agonist

Decongestion of mucous membranes and increase in BP

Used as a nasal decongestant, pressor, and for CNS stimulation

Side effects: CNS efects

Not metabolized by MAO or COMT

Relatively selective for Beta 2

Bronchodilation

Used in asthma

Side effects: high doses can activate Beta 1 and cause heart effects

A CNS stimulant that encourages the release of NE from the nerve terminal via facilitated exchange

Used in narcolepsy and weight reduction

Side effects: CNS stimulation, PV effects, risk of abuse

Not metabolized by MAO or COMT

CNS stimulant that encourage release of NE from the nerve terminal via faciliated exchange

Used in ADHD

Side effects: excess CNS stimulation, PV effects, risk of abuse

Inhibits PDE and adenosine to cause sympathomimetic effect without adrenergic receptor binding

Works downstream from cAMP to allow intracellular build up of NE

Causes sensitization of cortex, respiratory area, increased HR, contractility, dilation of BV, and cerebral vascular constriction

Used in alterness and relief of headache

Inhibits PDE and adenosine to cause sympathomimetic effect without adrenergic receptor binding

Works downstream from cAMP to allow intracellular build up of NE

Causes sensitization of cortex, respiratory area, increased HR, contractility, dilation of BV, and cerebral vascular constriction

Used bronchial asthma with Beta 2

Has less effects on heart and lungs, more CNS

Reversible selective Alpha 1 antagonist

Decreases BP with reflex tachycardia

Used in HTN and BPH

Side effects: postural hypotension, inhibition of ejaculation, nasal stuffiness

Irreversible selective Alpha 1 antagonist

Binds covalently for 24 hours

Used in pheochromocytoma (with propanolol)

Side effects: postural hypotension, reflex tachycardia, inhibition of ejaculation

Non-selective alpha antagonist

Alpha 1: decrease BP

Alpha 2: prevents feedback inhibition of NE

Causes greater reflex tachycardia due to Beta 1 stimulation

Used in pheochromocytoma with propanolol

Non-selective Beta antagonist

Beta 1: decrease HR, contractility, conduction, renin

Beta 2: increase TPR, slow recovery from hypoglycemia, increased TG/VLDL, increased airway resistance

Causes NET decrease in BP

Used in HTN, cardiac arrhythmias, angina, glaucoma, MI, Pheo, heart failure, performance anxiety

Side effects: decreased CO, heart block, bronchospasm, CNS effects

Non-selective Beta antagonist

Decrease in aqueous humor production

Same uses as Propanolol

Selective Beta 1 antagonist

Decreases HR, CO, conduction, renin

Also affects Beta 2 at high doses

Used for same reasons as propanolol

Same adverse effects as propanolol

Has less respiratory effects than non-selectives

Most selective Beta 1 antagonist

Same effects and indications of propanolol

Has an 8 minute half life

Less respiratory effects than non-selectives

Clonidine

Alpha 2 agonist

Binds to Alpha 2 to produce feedback inhibition of NE

Blocks sympathetic outflow

Used in essential HTN, reduction of opioid withdrawal, OAG, and ADHD

Side effects: dry mouth, sedation, HTN crisis

Binds to Alpha 2 to produce feedback inhibition of NE

Blocks sympathetic outflow

Used in essential HTN

Side effects: autoimmune response

Is a prodrug that is safe to use to pregnancy

Enters the pre-synaptic terminal via diffusion

Blocks VMAT and depletes NE

Enters the pre-synaptic terminal via the NET

Uncouples the AP from Ca entry

Concentrated in NE vesicles and depletes NE

Substrate for NET

Enters pre-synaptic nerve terminal

Displaces NE via facilitated exchange so that NE is release

Carbonic anhydrase inhibitor that works at the proximal tubule

Prevents reabsorption of HCO3-

Decreases H+ secretion

Decreases production of aqueous humor

Used in OAG, urinary alkalinization, metabolic alkalosis, acute mountain sickness, epilepsy

Side effects: hyperchloremic acidosis, hypersensitivity with sulfas

Urine: increased HCO3-, Na+, K+, decreased Cl-

Blood: increased H+

Most commonly used diuretic that works at the distal convoluted tubule

Inhibits the NaCl anti-port

Produces a hyperosmolar urine

Used in HTN, CHF, hypercalciuria, and nephrogenic DI

Works as ADH substitute

Side effects: hyperkalemia, hypercalcemia, hypochloremic acidosis, increased TG/VLDL

Urine: increased Na+, Cl-, K+, decreased Ca++

Blood: hypokalemia

Most efficaceous diuretic

Inhibits the NKCC and disrupts the positive lumen potential, causes diminished Mg and Ca reabsorption

Inhibits a concentrated or dilute urine

Decreases renal vascular resistance

Used in pulmonary edema, hyperkalemia, acute renal failure

Contraindicated with quinidine, hypersensitivity with sulfas

Urine: increased NaCl, K, H, Mg, Ca, HCO3-

Blood: hypokalemic alkalosis, hypochloremia

Aldosterone antagonist that only works in the presence of aldosterone

Prevents insertion of Na+ channels in CD

Used to retain K, aldosteronism

Side effects: hyperglycemia, gynecomastia, menstrual irregularities

Causes increased secretion of NaCl and hyperkalemia

K sparing diuretic that does not require aldosterone.

Works at the CD to block Na channels

Used in conjunction with furosemide or hydrochlorothiazide or prevent hypokalemia

Induces P450

An osmotic diuretic that is freely filtered

Works at water permeable segments (PT, DL, CD)

Increases osmotic activity of solute, preventing water reabsorption and favoring secretion

Increases RBF, and decreases corticomedullary gradient

Used in AKI, acute glaucoma, dialysis

Decreases osmolarity of urine

Non-peptide ADH antagonist that works at the collecting tubule basolateral membrane

Used in SIADH, hyponatremia, and CHF

Side effect: hypernatremia

Increased urine volume with decreased osmolarity

Chlorpheniramine

Diphenhydramine

Dimenhydrinate

Used in OTC medications, anti-motion sickness, and sleep aid

Loratadine

Fexofenadine

Metabolized by CYP3A4

Longer lasting

Less CNS effects

Used for allergic rhinitis

Cimetidine

Rantidine

Famotidine

Prevent histamine stimulated acid secretion

Used in ulcers, GERD, Zollinger-Ellison syndrome

Side effects: prolactin, impotence, gyncomastia

Can suppress first pass effect of alcohol

Prevents mast cell degranulation

Used in allergic rhinitis

Side effects: itching, sneezing, and headache