Medications Exam 1 with Physiology

What does stimulation of adrenergic Beta 2 receptors do?

Cause vasodilation of smooth muscle (an increase in blood flow), increase in bronchodilation (increase in oxygen flow), decrease in GI motility and slow digestion, and increase of secretions of aqueous humor to support and maintains shape of eyes. There is also an increase in glucose released into the blood, an increase in glucagon and an increase in lipoprotein lipase.

What receptors does Phenylephrine (sudafed PE) stimulate?

Activates alpha 1 adrenergic receptors

What type of medication is Phenylephrine (Sudafed PE)?

An Alpha 1 agonist

What receptors does Clonidine (Catapres) activate?

They activate Alpha 2 adrenergic receptors

What type of medication is Clonidine (Catapres)?

Alpha 2 Agonist

Indications for Phenylephrine (Sudafed PE)

Rhinitis- nasal decongestent by causing vasoconstriction of submucosal nasal blood vessels

Hypotension- It causes systemic vasoconstricition, which increases blood pressure. The body then compensates by lowering the heart rate and causing compensatory bradycardia

Mydriasis Induction- Used as a topical agent in opthalmological procedures

Side effects of Phenylephrine (Sudafed PE)

HTN, Stroke, MI

How does clonidine (Catapres) effect presynaptic neurons in medulla?

When given ORALLY, clonidine stimulates alpha 2 adrenergic receptors on the presynaptic neurons in the medulla by DECREASING NE release in sympathetic neurons, causing BP to lower

How does clonidine (Catapres) effect the prefrontal cortex

Decreases NE release, allowing the body to turn out irrelevant stimuli to sharpen focus, allowing the treatment of ADHD

What type of medication is isoprenaline?

A Non-selective beta agonist

What type of medication is albuterol (Proventil HFA)

Selective Beta 2 agonist

What type of medication is Salmeterol (Serevent)?

Selective beta 2 agonist

How does Isoproterenol (isoprenaline) work?

It works by acting on the Beta 1 and Beta 2 adrenergic receptors. This increases heart rate and contractility, causing the heart to work harder and pump more blood out, thus increasing oxygen and energy demands. It also activate beta 2 receptors in vessel walls, causing vasodilation and lowering peripheral vascular resistance

What are the indications for Isoproterenol (isoprenaline)?

Bradycardia and heart block

What are the side effects of Isoproterenol (isoprenaline)

Tachycardia, Palpitations, Arrhythmias, Angina pectis, and Myocardial Infarction

What are the contraindications of Isoproterenol (Isoprenaline)?

Coronary heart disease

What do selective beta 2 agonists do

Only activate beta 2 adrenergic receptors

What type of medication is albuterol (proventil HFA)

A short acting beta 2 agonist

What type of medication is almeterol (serevent diskus)

Long Acting beta 2 agonists

How does Albuterol and Salmeterol work?

They stimulate beta 2 receptors in airway smooth muscles by causing bronchodilation

What are the indications for albuterol and salmeterol?

Asthma and COPD

What are the side effects of Albuterol and Salmeterol?

Tachycardia, Dysrhythmias, and tremors

What type of medication is Epinephrine (EpiPen)

A Sympathomimetic (mimics the effects of the sympathetic nervous system, which controls the body's "fight-or-flight" response)

What does Epinephrine (EpiPen) act on

It acts on both alpha and beta adrenergic receptors

How does epinephrine (EpiPen) act on the body

It causes vasoconstriction by acting on alpha adrenergic receptors and causes relaxation of bronchial smooth muscles by triggering beta adrenergic receptors. It also causes relaxation of the smooth muscle of the stomach, intestine, uterus, and urinary bladder

Indications of epinephrine (EpiPen)

Anaphylaxis, asthma exacerbation (severe), septic shock, and ACLS (Advanced Cardiovascular Life Support)

Side effects of Epinephrine (EpiPen)

Palpitations/Tachycardia/Arrhythmias, HTN, nausea, vomitting, dizziness, tremor, nervousness, and anxiety

What type of receptors are adrenergic receptors?

G protein coupled receptors that bind catecholamines, such as epinephrine and norepinephrine

What receptor cells does alpha 1 have on target organ

Gq cells, Epinephrine, and Norepinephrine

What receptors does Alpha 2 have on target organ

Gi, Norepinephrine, and Epinephrine

What type of receptors does Beta 1 have on target organ

Gs, Norepinephrine, and Epinephrine

What type of receptors does beta 2 have on target organ

Gs and Epinephrine

What type of receptors does Beta 3 have on target organ

Gs and Epinephrine

How do andrenergic receptors effect the body

by triggering the sympathetic division, they cause

pupil dilation,

inhibit salivation,

accelerate heart beat,

facilitate breathing,

inhibit digestion,

stimulate release of glucose,

secrete epinephrine and norepinephrine,

relax bladder,

and inhibit sex organs

What are adrenergic antagonists also known as

Sympatholytics

Locations of alpha 1 receptors and their correlating actions

most vascular smooth arrow (innervated)- contraction

Pupillary dilator muscle- contraction causing pupil dilation

Pilomotor smooth muscle- erects hair

Prostate- contraction

Heart- increases force of contraction

Location and correlating action of Alpha 2 adrenergic receptors

Postsynaptic CNS neurons- multiple actions

Platelets- aggregation

Adrenergic and cholinergic nerve terminals- inhibits transmitter release

Some vascular smooth muscle- contraction

Fat cells- inhibits lipolysis

Location and correlating actions of Beta 1 receptors

Heart, Juxtaglomerular cells- increase force and rate of contraction, increase renin release

Location and correlating actions of Beta 2 receptors

Respiratory, uterine, and vascular smooth muscle- promotes smooth muscle relaxation

Vascular smooth muscle supplying brain and skeletal muscle- vasodilation

Skeletal muscle- promotes potassium uptake

Liver- activates glycogenolysis, causing an increase in blood glucose levels

Location and correlating actions of Beta 3

Bladder- relaxes detrusor muscle

Fat cells- Activate lipolysis, causing the increase in break down of triglycerides into free fatty acids and cholesterol

Location and correlating actions of Delta 1 receptors

Smooth muscle- dilates renal blood vessels

Location and correlating actions of Delta 2

Nerve endings- modulates transmitter release

What type of medicine is Phenylephrine and Methoxamine

Alpha agonist

What receptors does Phenylephrine and Methoxamine bind to

Alpha 1 receptors

What type of medication is Clonidine and Methylnorepinephrine

Alpha agonist

What receptors does Clonidine and Methylnorepinephrine react with

Alpha 2 receptors

What type of medications are Norepinephrine and Epinephrine

Mixed alpha and beta agonists

What receptors does Norepinephrine react with

Alpha 1 and Alpha 2, and more so Beta 1 than Beta 2

What receptors does Epinephrine react with

Alpha 1, Alpha 2, Beta 1, and Beta 2

What type of medication is Dobutamine

Beta agonist

What type of medication is Isoproterenol

Beta agonist

What type of medication is Albuterol

Beta Agonist

What type of medication is Terbutaline

Beta Agonist

What type of medication is Metaproterenol

Beta Agonist

What type of medication is Ritodrine

Beta agonist

Tell me about dobutamine

receptors reacts to is Beta 1

Tell me about Isoproterenol

It interacts with beta 1 and beta 2 receptors about equally/equally

Tell me about Albuterol, Terbutaline, Metaproterenol, and Ritodrine

They interact with Beta 2 receptors

What type of medication is Dopamine

It is a dopamine agonist

What type of medication is Fenoldopam

Dopamine agonist

Tell me about Dopamine

Reacts with both D1 and D2 receptors about equally/fully equally

Tell me about Fenoldopam

It reacts with D1 receptors more than D2 receptors (aka it acts on D1 receptors)

Tell me about phenoxybenzamine (Dibenzyline)

It is a non selective alpha blocker that acts on Alpha 1 and Alpha 2 adrenergic receptors

Tell me about Phentolamine (Regitine)

It is a non selective Alpha Blocker that acts on Alpha 1 and Alpha 2 adrenergic receptors

Tell me about Doxazosin (Cardura)

It is a selective Alpha 1 blocker that acts on Alpha 1 adrenergic receptors

Tell me about terazosin (Hytrin)

It is a selective Alpha 1 blocker that acts on Alpha 1 adrenergic receptors

Tell me about propanolol (Inderal)

It is a nonselective beta blocker

Tell me about atenolol (tenormin)

It is a cardioselective beta blocker

Tell me about metoprolol tartate (Lopressor)

It is a cardioselective beta blocker

Tell me about labetalol (Trandate)

It is a Alpha Beta (type of beta) blocker

Tell me about Carvedilol (Coreg)

It is an Alpha Beta (type of beta) blocker

Tell me about how non selective alpha blockers

They act on alpha 1 and alpha 2 adrenergic receptors to block alpha 1 receptors→ vasodilation→ lowers BP

Describe phenoxybenzamine aka Dibenzyline (descriptor, synthesis, and uses)

Irreversible, noncompetitive antagonist

Synthesize new adrenergic receptors every 24 hours

Used in treatment of Pheochomocytoma

Describe phentolamine aka Regitine (descriptor and indications

Competitive antagonist

Can be used in treatment of pheochromocytoma (but not typically) and used in Hypertensive crisis caused by MAOI with tyramine rich food/drink

Side effects of Non Selective Alpha Blockers

By inhibiting Alpha 1, you cause vasodilation. This vasodilation can cause hypotension, headache (in brain), nasal congestion (in nasal mucosa), and difficulty ejaculating (in seminal tract)

Also causes:

Tachycardia (BP drops causing increase in HR)

Uncontrolled catecholamine release (inhibition of A2 receptors in presynaptic neurons)

Arrythmia (excess catecholamines act on beta receptors too which inc. HR causing tachycardia which can lead to arrythmia)

What does doxazosin (Cardura) block

block NE and Epinephrine from binding to A1

What does terazosin (Hytrin) do side effect wise

less severe side effect due to negative feed inhibition through A2 adrenergic receptors still working

Indications of doxazosin (Cardura) and terazosin (Hytrin) aka A1 blockers

Hypertension (excluding 1st line) and Urinary retention secondary to BPH

Tell me about propanolol (Inderal)

A non selective beta blocker of First gen. beta blockers

Is an Antagonist on both beta 1 and beta 2 adrenergic receptors

What happens if you block Beta 1 receptors

Heart: Dec. HR, Dec. Contractility→ heart works less hard and pumps less blood out→ dec. in O2 and energy demands and dec. BP

Juxtaglomerular cells in kidney: dec. renin release→ dec. Angiotensin 2 and Aldosterone→ loss of Na+ and H2O in urine→ dec. BP

What happens if you block Beta 2 receptors

Some vasoconstriction of blood vessels supplying skeletal muscle and brain occurs

ONLY propanolol (Inderal) can reach B2 receptors in brain bc it is lipid soluble enough to penetrate blood brain barrier to induce some degree of vasoconstriction

What happens in the body if you block Beta 2 receptors

Lungs- bronchoconstriction

GI tract- inc. motility

Eyes- dec. production of aqueous humor→ dec intraocular pressure

Liver- dec. glucose release in blood

Pancreas- decreases release of glucagon → dec. blood glucose level

Inhibition of lipoprotein lipase- inc. accumulation of triglycerides in blood

Indications of propanolol (Inderal)

Hypertension

Coronary artery disease (Angina pectoris, post MI to dec. risk of another cardiovascular event)

Severe tachycardia from thyroid storm

Severe tachycardia from anxiety

Prevention of migraines

side effects of propanolol (Inderal)

Bradycardia

Hypotension

Rebound tachycardia, HTN, arrythmias from abrupt cessation

Fatigue

Dizziness, depression, insomnia, nightmares

Bronchospasm- wheezing, SOB, chest tightness

Hypertriglyceridemia

Hypoglycemia

(it’s a non selective beta blocker))

Contraindications of propanolol (Inderal)

Asthma

COPD

Take PRECAUTION for patients wit diabetic patients taking hypoglycemic agents (insulin)

Name 2 second generation beta blockers

Atenolol (Tenormin)

Metoprolol Tartate (Lopressor)

Describe atenolol (Tenormin) and metoprolol tartate (Lopressor)

Cardioselective beta blockers

Selective for Beta 1 adrenergic receptors

Lower BP by decreasing HR and contractility

In kidneys, dec. release of renin

Indications for Atenolol (Tenormin) and metoprolol tartate (Lopressor)

HTN

Angina

Cardiovascular event risk reduction post MI

Acute MI (specifically metoprolol tartate/Lopressor)

Side effects of Atenolol (Tenormin) and metoprolol tartate (Lopressor)

Bradycardia

Hypotension

Rebound tachycardia, HTN, and arrhythmias from abrupt cessation

Describe uses Atenolol (Tenormin) and metoprolol tartate (Lopressor)

Because they don’t block B2 receptors

Don’t cause bronchoconstriction- safe for patients with COPD and asthma

Less effects on blood glucose- preferred for diabetic patients

Note: at high enough doses, Atenolol (Tenormin) and metoprolol tartate (Lopressor) may also start to block B2 receptors

What generation of Beta blockers are labetalol (Trandate) and carvedilol (Coreg)

Third generation beta blockers

What type of beta blockers are labetalol (Trandate) and carvedilol (Coreg)

Alpha Beta Blockers

Tell me about labetalol (Trandate) and carvedilol (Coreg) (Mechanism of Action)

Block B1 receptors and A1 receptors in blood vessels that normally cause vasoconstriction

When are labetalol (Trandate) and carvedilol (Coreg) used

Works for HTN treatment where vasoconstriction is an issue (like patients with peripheral vascular disease)

Indications for labetalol (Trandate)

Chronic hypertension in pregnancy

IV administration in hypertensive emergency

Indications for carvedilol (Coreg) and WHY

Due to antioxidant properties:

Dec. free radical production to prevent thickening of blood vessel walls

Dec. Atherosclerosis

Helps treat Heart Failure

Side effects of labetalol (Trandate) and carvedilol (Coreg) and WHY

Orthostatic hypotension due to blocking of alpha receptors

What do muscarinic antagonists do (aka antimuscarinics)

Block rest and digest

What type of medication is atropine

muscarinic antagonist

What type of medication is oxybutynin (Ditropan)

muscarinic antagonist