Bethanechol (Urecholine®)

Drug Class

MOA

Therapeutic Use

Side Effects

Drug Class/Category:

Direct-Acting Cholinergic Agonist (a.k.a. - parasympathomimetic).

MOA:

Binds directly to and stimulates the cholinergic receptor (M), and mimics the actions of Ach.

Therapeutic Use:

i. Reflux esophagitis

ii. Urinary retention (post operative, post partum)

iii. Post operative ileus

Side Effects: 

BBSMUDGE

Neostigmine (Prostigmin®)

Drug Class

MOA

Therapeutic Use

Side Effects

Drug Class/Category:

Indirect-Acting Cholinergic Agonist (a.k.a. - Anticholinesterase)

MOA:

Inhibits acetylcholinesterase, → accumulation or ↑ of ACh at all cholinergic receptor s, including neuroeffector junction. Indirectly enables ACh to work at the (M) & (NM) sites.

Therapeutic Use:

i. Myasthenia gravis

ii. Urinary retention (post partum)

iii. Post operative ileus

iv. Antidote to excessive cholinergic blockade

Side Effects:

BBSMUDGE

Atropine (generic tablets and injectable) 

Drug Class

MOA

Clinical Indications

Side Effects

Drug Class/Category:

Anti-Cholinergic Drug (a.k.a. - Parasympatholytics)

MOA: 

Binds to the M receptors, without stimulating, and blocks ACh from binding to the receptor (competitive antagonism).

Clinical Indications: 

i. Antisecretory effects prior to surgery & in asthma or COPD

ii. Bronchodilating effects in asthma & COPD

iii. Antidote for cholinesterase inhibitor toxicity (i.e., organophosphate pesticides, physostigmine)

Side Effects:

Tachycardia, Dry Mouth, Blurred vision (mydriasis), Urinary retention, Flushing/redness & dryness of skin, Fever (hyperpyrexia), CNS effects (stimulation, depression, drowsiness)

Ipratropium (Atrovent®)

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category:

Anti-Cholinergic Drug (a.k.a. - Parasympatholytics

MOA:

Binds to the M receptors, without stimulating, and blocks ACh from binding to the receptor (competitive antagonism). 

Clinical Indications:

• Inhalational drug (e.g., nebulized, metered dose inhaler) in the treatment of asthma & COPD to achieve bronchodilation

Side Effects:

Similar to Atropine

Other Critical info:

Synthetic analog of atropine that is less irritating to the bronchial smooth muscle

Isoproterenol (Isuprel®)

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category:

Direct Acting Beta Adrenergic Agonist (a.k.a. - Sympathomimetics)

MOA:

Binds directly to adrenergic receptors (b1 , b2 ) and mimics the actions of norepinephrine or epinephrine. 

Clinical Indications:

• Bronchodilation in asthma (b2 )

• In cardiac arrest for emergency stimulation of the heart (b1 ) 

Side Effects:

• Hypertensive Crisis (Hypertension, Cerebral Hemorrhage, Arrhythmias)

• Overstimulation of the heart (Palpitations, Arrhythmias)

Other Critical info: 

Non-subtype-selective for the b receptors (activates both b1 , b2 )

Albuterol (Ventolin®,Proventil®)

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category:

Direct Acting Beta 2 Adrenergic Agonist (a.k.a. - Sympathomimetics)

MOA:

Binds directly to adrenergic receptors (b2 ) to mimic the actions of norepinephrine or epinephrine.

Clinical Indications:

• Bronchospasm & Asthma (b2)

• Premature labor (b2 on uterus smooth muscle) 

Side Effects: 

• Hypertensive Crisis (Hypertension, Cerebral Hemorrhage, Arrhythmias)

• Overstimulation of the heart (Palpitations, Arrhythmias)

Other Critical info:

b2 selective adrenergic agonist (specific for b2 )

Phenylephrine (NeoSynephrine®)

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category:

Direct Acting Alpha-Adrenergic Agonist (a.k.a. - Sympathomimetics) 

MOA:

Binds directly to adrenergic receptors (a1 ) to mimic the actions of norepinephrine or epinephrine.

Clinical Indications:

• Increase BP (a1 )

• Nasal Decongestant (a1 on vessel smooth muscle) 

Side Effects:

• Hypertensive Crisis (Hypertension, Cerebral Hemorrhage, Arrhythmias)

• Overstimulation of the heart (Palpitations, Arrhythmias)

Other Critical Info:

a1 selective adrenergic agonist (specific for a1 )

Phentolamine (Regitine®)

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category:

Alpha-Adrenergic Blocking Drug (a.k.a.- adrenergic antagonist," a blocker")

MOA:

Bind to adrenergic receptors (a1 , a2 ), without simulating, and prevents NE and EPI from binding to the receptors (competitive antagonism). 

Clinical Indications:

• Pheochromocytoma (both a1 & a2)

Side Effects:

• Cardiovascular Effects (Bradycardia, Hypotension with compensatory tachycardia, Orthostatic hypotension, Fainting)

• Nasal Congestion 

Other Critical info:

Non-subtype-selective a adrenergic blocker (a1 , a2 )

Doxazosin (Cardura®)

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category: 

Alpha-Adrenergic Blocking Drugs (a.k.a.- adrenergic antagonist,"a blocker")

MOA: 

Bind to adrenergic receptors (a1 ), without simulating, and prevents NE and EPI from binding to the receptors (competitive antagonism).

Clinical Indications:  They block a1 

• hypertension (HTN)

• BPH 

Side Effects:

• Cardiovascular Effects (Bradycardia, Hypotension with compensatory tachycardia, Orthostatic hypotension, Fainting)

• Nasal Congestion

Other Critical info:

selective a1 adrenergic blocker

Tamsulosin (Flomax®)

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category:

Alpha-Adrenergic Blocking Drugs (a.k.a.- adrenergic antagonist,"a blocker")

MOA:

Bind to adrenergic receptors (a1A), without simulating, and prevents NE and EPI from binding to the receptor (competitive antagonism).

Clinical Indications:  (blocks a1A)

• BPH

Side Effects: 

• Potential for Cardiovascular Effects as with Doxazosin and Terazosin, but less risk 

Other Critical info:

selective blocker of the a1A subtype found exclusively in bladder smooth muscle)

Atenolol (Tenormin®) 

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category:

Beta - Adrenergic Blocking Drugs (a.k.a.- adrenergic antagonist," b blocker")

MOA:

Bind to adrenergic receptors (b1 ), without simulating, and prevents NE and EPI from binding to the receptors (competitive antagonism). 

Clinical Indications:

•HTN , Angina Pectoris, & CHF (over long term with proper doses)

↓HR -> ↓ HEART OVER WORK 

Side Effects:

• Cardiovascular Effects (Hypotension , Bradycardia, CHF & Cardiac Arrest if overdosed)

• Better versus propranolol in NOT CAUSING brochoconstriction due to being “cardioselective” 

Other Critical info:

Second Generation b1 selective adrenergic blocker (“Cardioselective b blockers”)

Atracurium (Tracrium®)

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category:

Peripheral Skeletal Muscle Relaxant (a.k.a. – NMJ blocker)

MOA:

Direct binding with NM receptor without stimulating the receptor (“occupying”), so ACh cannot bind and stimulate

Clinical Indications:

• To relax abdominal or intrathoracic skeletal muscles before surgery (premedication) and during surgery (surgical relaxation)

• Airway management in emergencies

• In ICU setting to ventilate critically ill patients with COPD or bronchospasms

• Diagnostic procedures (e.g., laryngoscopy)

Side Effects:

• Paralysis of the respiratory muscles

• Bronchospasm & increased respiratory secretions (histamine related)

Other Critical info:

• Non-Depolarizing Peripheral Skeletal Muscle Relaxants

• essentially results in a gradual paralysis 

Theophylline (aminophylline, Theo-Dur®)

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category:

Bronchodilating Agent

MOA: 

relaxes the smooth muscle of the bronchioles through its inhibition of phosphodiesterase

Clinical Indications: 

•Asthma

•COPD 

Side Effects:

• Excessive cardiac and CNS stimulation 

Other Critical info:

• Once mainstay in asthma treatment, now largely replaced by b -agonists and corticosteroids

• Narrow Therapeutic Index (Dose must therefore be adjusted carefully)

Mometasone (Asmanex®, Nasonex®)

Drug Class

MOA

Clinical Indications

Side Effects

Other Critical Information

Drug Class/Category:

Corticosteroid Antiinflammatory Agent 

MOA:

Prolonged (months) inhalation of corticosteroids interferes with all stages of the inflammatory response (results in ↓ in number of immune cells; in reduced hyper-responsiveness; and inhibited release of mediators)

Clinical Indications:

•Asthma

•COPD

Other Critical info:

Has no direct dilating effect on the airway smooth muscle

Eyes - Sympathetic

Receptor

Effects

alpha 1

pupils dilate (mydriasis)

Eyes - Parasympathetic

Receptor

Effects

M

pupils constrict (miosis)

Lungs - Sympathetic

Receptor

Effects

beta 2

Trachea & bronchioles dilate/relax

Think OPEN UP - Max Oxygen

Lungs Parasympathetic

Receptor

Effects

M

Trachea & Bronchioles constriction; secretions are up; comfortable/restful state

Bladder - Sympathetic

Receptor

Effects

alpha 1

Bladder sphinter and trigone muscles contract; detruser muscle relaxes

Bladder - Parasympathetic

Receptor

Effects

M

Bladder sphincter & trigone muscles relax; detruser muscle contracts

Heart - Sympathetic

Receptor

Effects

beta 1

Heart rate increases

Force of Contraction (FOC) increases

Heart - Parasympathetic

Receptor

Effects

M

Heart rate decreases

Force of Contraction Decreases

Intestines - Sympathetic

Receptor

Effects

alpha 1

Decreased

GI tone, motility & sphincter contraction

Intestines - Parasympathetic

Receptor

Effects

M

Increased

GI tone, motility & sphincter contraction

Blood Vessels - Sympathetic

Receptors

Effects

alpha 1

vasoconstriction

beta 2 

vasodilation

BOTH are SYMPATHETIC

In Females - Uterus - Sympathetic

Receptors

Effects

alpha 1

uterine muscle constriction

beta 2

uterine muscle relaxation

BOTH are SYMPATHETIC

(check with Santana)

Cholinergic Drugs

Direct Acting (AKA as)

MOA

Drugs

Side Effects

Parasympathomimetics

MOA: 

Bind directly to & stimulate M receptors

Drugs:

Acetylcholine

Bethanechol

Pilocarpine

BBSMUDG

Bradycardia & hypotension

Bronchoconstriction

Salivation

Miosis (pupil constriction)

Urinary Urgency

Diaphoresis (sweating)

GI Disturbances (N/V/D)

(cholinergic crisis) ?

Cholinergic Drugs

Indirect Acting (AKA)

MOA

Drugs

Side Effects

Antocholinesterases

MOA:

Inhibit the action of acetylcholinesterase which allows ACh to accumulate and stimulate M and N receptors.

Drugs:

Physostigmine

Neostigmine

Side Effects:

BBSMUG (say all)

Cholinergic Drugs

Anticholinergics (AKA)

MOA

Drugs

Side Effects

Parasympatholytics

MOA:

Competitive Antagonist with ACh for M receptors

Drugs:

Atropine

Ipratroprium

Dicyclomine

Side Effects:

Caused by excessive blockage of parasympathetic system

Opposite of BBSMUDG (so name them!)

Tachycardia

Dry Mouth

Mydriasis (pupils dilate)

Urinary Retention

Flushing/Redness/Dry skin

Fever

CNS effects (stimulation, depression, drowsiness)