1.  epinephrine (generic; Adrenaline)

2.  Norepinephrine (generic; Levophed)

3.  Isoproterenol (generic; Isuprel)

4.  Dopamine (Dopar; Larodopa)

1.  Tyramine

2.  Amphetamine (generic)

3.  Methamphetamine (Desoxyn)

4.  Methylphenidate (generic; Ritalin)

5.  Ephedrine (generic)

6.  Phenylephrine (generic; Neo-synephrine)

7.  Methoxamine (Vasoxyl)

1.  Metaproterenol (Alupent; generic)

2.  Terbutaline (Brethine; Bricanyl)

3.  Albuterol (generic; Proventil; Ventolin; others)

4.  Salmeterol (serevent)

5.  Ritodrine (generic)

6.  Dobutamine (generic; Dobutrex)

1.  cocaine

2.  Tricyclic antidepressants

1.  clinidine (generic; Catapres)

2.  alpha-methyl DOPA (generic)

3.  alpha-methyl-para-tyrosine

4.  Reserpine (generic)

5.  Guanethidine (Ismelin)

1.  clonidine (generic; Catapres)

2.  alpha-methyl DOPA (generic)

1.  reserpine (generic)

2.  Guanethidine (ismelin)

1.  phentolamine

2.  phenoxybenzamine

3.  prazosin

4.  doxazosin

5.  terazosin

6.  yohimbine

1.  propranolol (generic; Inderal)

2.  Metoprolol (generic; Lopressor)

3.  Atenolol (generic; Tenormin)

4.  Pindolol (generic; Visken)

5.  Timolol (generic; Blocadren)

6.  Nadolol (generic; Corgard)

7.  Betaxolol (Kerlone)

8.  Esmolol (BreviBloc)

1.  Labetalol (generic; Normodyne; Trandate)

2.  Carvedilol (Cartrol)

epinephrine

1.  Type

2.  Where it comes from?

3.  What receptors does it act on?

4.  How is it administered?

1.  Catecholamine

2.  chromaffin cells of the adrenal medulla (not from peripheral nerve endings).  It is also released in the CNS as a neurotransmitter.

3.  acts on all alpha and beta adrenoceptors. 

4.  parenterally or by inhalation

norepinephrine

1.  Type

2.  Which receptors does it act on?

1.  catecholamine

2.  all alpha adrenoceptors as well as beta 1 adrenoceptors

Isoproterenol

1.  Type

2.  Which receptors does it act on?

3.  Uses

1.  Synthetic catecholamine

2.  pure beta-adrenergic stimulant

3.  relieve bronchoconstrictive states with the cardiovascular effects usually being untoward side effects.

dopamine

1.  Type

2.  Where does this act?

3.  Uses

1.  Catecholamine

2.  acts in the CNS (important in the xtrapyramidal motor system).  Renal blood vessels possess non-innervated dopamine receptors that produce vasodilation in the kidney

3.  deficiency causes Parkinson's disease, so we administer L-DOPA for treatment.

tyramine

1.  Type

2.  Effects on the body

1.  Non-catecholamine sympathomimetic (alpha adrenoceptor agonists)

2.  Causes a massive release of NE from sympathetic nerve endings.  This may cause hypertensive crisis in patients who are taking an MAO inhibitor to treat depression (MAO inactivates tyramine)

With a massive release of NE, this can cause an increase in blood pressure.

amphetamine

1.  Type

2.  Uses

3.  Side Effects

1.  non-catecholamine sympathomimetic (alpha-adrenoceptor agonist)

2.  Orally effective and readily enters the CNS.  Temporary elevation of mood and appetite suppression.

3.  Highly toxic and lethal.  Due to tolerance, the ED50 increases, but the LD50 remains unchanged.  If they die, the major find at autopsy is cerebral hemorrhage that may be secondary to intense vasoconstriction of CNS blood vessels

Note:  indicated in treatment of hyperkinetic children or narcolepsy.

methamphetamine

1.  Type

2.  Uses

3.  Side Effects

1.  non-catecholamine sympathomimetic (alpha-adrenoceptor agonist)

2.  Orally effective and readily enters the CNS.  Temporary elevation of mood and appetite suppression.

3.  Highly toxic and lethal.  Due to tolerance, the ED50 increases, but the LD50 remains unchanged.  If they die, the major find at autopsy is cerebral hemorrhage that may be secondary to intense vasoconstriction of CNS blood vessels

methylphenidate

1.  Type

2.  Uses

3.  Side Effects

1.  non-catecholamine sympathomimetics (alpha-adrenoceptor agonist)

2.  CNS stimulant.  This is Ritalin and is used in the treatment of children with ADHD.

3.  CNS excitation and convulsions

ephedrine

1.  Type

2.  Uses

3.  Side Effects

4.  Which receptors does it act on?

1.  non-catecholinamine sympathomimetics (alpha adrenoceptor agonist)

2. Oral treatment for bronchial asthma (Beta effect) and is found in over-the-counter medications for ear and nasal decongestion.  It has also been used for its alpha effects as a pressor agent.  Also, in ophthalmology to produce short lasting mydriasis without cycloplegia.

3. Didn't list any but I'm sure you can think of something

4.  acts as an agonist to all alpha and beta receptors in the body

Phenylephrine (Neo-synephrine)

1.  Type

2.  Uses

3.  Side Effects

1.  non-catecholamine sympathomimetic (alpha adrenoceptor agonist)

2.  orally effect in extremely large doses but it is in some over-the-counter cold medications (questionable).  it is a pressor agent and is used to produce mydriasis in ophthalmology.  Used in nasal spray to produce local vasoconstriction in nasal airways (like Afrin with rebound)

Methoxamine

1.  Type

2.  Uses

1.  non-catecholamine sympathomimetic (alpha-adrenoceptor agonist)

2.  administered parenterally as a pressor drug; used to produce mydriasis and sometimes to treat paroxysmal atrial tachycardia (via production of reflex bradycardia)

Metaproterenol

1.  Type

2.  Which receptor does it target?

3.  Uses

4.  Side Effects

1.  non-catecholamine sympathomimetic (beta-adrenoceptor agonist)

2.  selective for beta 2 adrenoceptors

3.  Used to treat bronchial asthma.  It can be administered by inhalation or orally. 

4.  Cardiac side effects may be seen as they have some beta 1 adrenoceptor stimulating activity.

Terbutaline

1.  Type

2.  Uses

3.  Side effects

1.  Non-catecholamine sympathomimetic (beta-adrenoceptor agonist)

2.  Used to prevent premature child birth

3.  It is a modification of metaproterenol but is longer lasting and has higher incidence of cardiac side effects.

Albuterol

1.  Type

2.  Uses

1.  Non-catecholamine sympathomimetic (beta-adrenoceptor agonist)

2.  asthma treatment (similar to terbutaline).  It is long acting with fewer cardiac effects than terbutaline.

Ritodrine

1.  Type

2.  Uses

3.  Side Effects

1.  beta-adrenoceptor agonist (selective for beta 2)

2.  use to relax smooth muscle of uterus and delay premature labor. 

3.  possible cardiac side effects

Dobutamine

1.  Type

2.  Uses

3.  Side effects

1.  Beta-adrenoceptor agonist (selective for Beta 1)

2.  Increases cardiac output without vasoconstriction.  It increases the force of contraction with much less effort on heart rate and conduction.

3.  It is rapidly metabolized by the liver, thus it must be given IV under close supervision.

Cocaine

1.  Type

2.  Uses

1.  Indirectly acting sympathomimetics

2.  Sometimes used for severe depression.  They block NE reuptake as their primary mode of action.  This is often used as a local anesthetic.

Tricyclic antidepressants

1.  Type

2.  Uses

1.  Potent inhibitor of catecholamine reuptake in adrenergic nerve terminals

2.  Used for their CNS effects in treating pathological depression

Guanethidine (ismelin)

1.  Type

2.  Uses

1.  Blocker of adrenergic nerve function (catecholamine depletion in the peripheral sympathetic nerve endings).  It does this by preventing the nerve action potential from invading the fine nerve terminals so that NE is not released (blocker of action potentials).  It can also displace the stored NT.

2.  potent antihypertensive drug.  It does not pass the blood-brain barrier so it cannot get into the CNS.

6-OH dopamine

1.  Type

2.  Uses

1. cytodestructor of nerve terminals

2.  experimental; pumped into sympathetic neurons and it destroys nerve terminals.

Clonidine

1.  Type

2.  Uses

3.  Side effects

1.  CNS acting sympatho-inhibitory agent on alpha 2 receptor

2.  antihypertensive drug; readily penetrates into CNS where it acts to decrease sympathetic tone to the blood vessels and to the heart.  It may also act in the CNS to enhance vagal outflow to the heart by potentiating baroreceptor mechanisms.  Also used in withdrawal treatment from opioid and ethanol addiction. 

alpha-methyl DOPA

1.  Type

2.  Uses

1.  CNS acting sympatho-inhibitory agent

2.  antihypertensive agent; crosses the blood brain barrier and in the CNS is converted to alpha-methyldopamine and then to alpha-methylnorepinephrine that is a potent alpha 2 adrenoceptor agonist.

alpha-methyl-para-tyrosine

1.  Type

2.  Uses

1.  this is a tyrosine hydroxylase inhibitor (decreases the amt of NE)

2.  reduces transmitter concentration in sympathetic post-ganglionic fibers.  It is occassionally used to depress catecholamine levels in patients with a pheochromocytoma prior to surgery

Reserpine

1.  Type

2.  Uses

3.  side effects

1.  catecholamine depletion.  interrupts the vesicular storage mechanism in sympathetic nerves. 

2.antihypertensive drug

3.  Will enter CNS and deplete all monoaminergic NT (NE, EPI, dopamine, serotonin); sedation; Parkinson's like syndrome

Phentolamine

1.  Type

2.  Uses

3.  side effects

1.  alpha antagonist (prefers the alpha 1 receptor)

2.  In the past, used for screening test for pheochromocytoma for pts with high plasma levels of catecholamines (alpha antagonist is better therapy than beta agonist or something like that)

3.  releases histamine that produces many false positive rxns.

Phenoxybenzamine

1.  Type

2.  How does it work?

1.  alpha-adrenoceptor agonist (preference for alpha 1 receptor)

2.  At first it is a competitive antagonist, but it also has the capcity to irreversibly bind to receptors because he is a beta-haloalkylamine

Prazosin

1.  Type

2.  Uses

3.  Side Effect

1.  Alpha-adrenoceptor antagonist (especially alpha 1 receptors)

2. Treatment of hypertensive pts.

3.  Does not produce large reflex tachycardia seen with other alpha-adrenoceptor antagonists.  Some pts have extreme hypotensive effect and loss of consciousness during first dose.

Note:  It may act in the CNS to depress sympathetic tone and cardiovascular reflex mechanism.  This is why we may not see the strong reflex tachycardia.

Terazosin and Doxazosin

1.  Type

2.  Uses

1.  Alpha-adrenoceptor antagonist

2.  prazosin-like drugs with longer half life which permits once a day dosing. Used to treat symptoms of benign prostatic hypertrophy

Yohimbine

1.  Type

2.  Uses

1.  alpha-adrenoceptor antagonist (selective for alpha 2)

2.  Used in experimental studies in pts with spinal cord damage.  Prevents CNS hypotensive effects of clonidine and alpha-methyldopa.

Propranolol

1.  Type

2.  Uses

1.  Beta-adrenoceptor antagonist (both beta 1 and beta 2)

2.  cardiac arrhythmias, potent local anesthetic, antihypertensive drug

Note:  metabolized by liver and elimination is through hepatic metabolism

Metoprolol

1.  Type

2.  Uses

3.  side effects

1.  Beta-adrenoceptor antagonist (selective for beta 1)

2.  reduces plasma renin

3.  less local anesthetic effects than propranolol but produces more CNS side effects including fatigue, dizziness, headache, and insomnia

Note:  eliminated in liver

Atenolol

1.  Type

2.  Uses

3.  side effects

1.  beta-adrenoceptor antagonist (selective for beta 1)

2.  usual beta 1 things.  Has a longer half life than metoprolol.

3.  Less CNS side effects than with metoprolol.  Can cause kidney problems because it is excreted in kidney.  Do not give to patients with severe renal disease

Pindolol

1.  Type

2.  Uses

1.  beta-adrenoceptor antagonist

2.  it has intrinsic sympathomimetic activity which means that it also stimulates the beta 1 adrenoceptors.  Therefore, it produces less cardiac depression and is better tolerated during exercise

Timolol

1.  Type

2.  Uses

1.  Beta-adrenoceptor antagonist

2.  Topical application produces a dramatic decrease in intraocular pressure.  This has become the drug of choice in treatment of open angle glaucoma.  Also clinically shown to be effective in preventing reinfarction of the myocardium.

Nadolol

1.  Type

2.  Elimination

1.  Beta-adrenoceptor antagonist

2.  excreted primarily by the kidney and has a long duration of action

Betaxolol

1.  Type

2.  Elimination

1.  beta-adrenoceptor antagonist (selective for Beta 1)

2.  metabolized by the liver but still has a long half life

Esmolol

1.  Type

2.  Uses

3.  Metabolism

1.  beta-adrenoceptor antagonist (selective for beta 1)

2.  acute emergency control of ventricular heart rate in patients with atrial fibrillation or atrial flutter (particularly those arrhythmias resulting from intraoperative anesthesia)

3.  Ultrashort half-life is due to rapid hydrolysis of cytosolic red blood cell esterases

Labetalol

1.  Type

2.  Uses

1.  alpha and beta antagonist (non-selective beta antagonist and alpha 1 antagonist)

2.  decreases plasma renin.  It is an effective antihypertensive agent that decreases total peripheral resistance with little reflex effect on the heart rate or cardiac output.  postural (orthostatic) hypotension is a problem in some pts.

Carvedilol

1.  Type

2.  Uses

1.  beta and alpha andrenoceptor antagonist

2.  free radical scavenger that may protect heart cells from damage.  Treats patients with congestive heart failure.

1.  Tyrosine (tyrosine hydroxylase)

2.  DOPA (DOPA decarboxylase)

3.  Dopamine (Dopamine beta-hydroxylase)

4.  Norepinephrine (phenylethanolamine N-methyltransferase)

5.  Epinephrine (this last step doesn't occur at the nerve endings)

Note:  The enzymes that are in paratheses tell us what enzyme take that molecule to the next step.  For example, tyrosine hydroxylase converts tyrosine to DOPA.

phenyl glycol

MAO is used to get it there.

low dose = decrease in blood pressure due to vasodilation.  This is because beta2 adrenoceptors are fewer in number but more sensitive than alpha adrenoceptors. 

high dose = increase in blood pressure due to vasoconstriction and vasoresponse.  This is because alpha adrenoceptors are more numerous but not as sensitive as beta 2 receptors.

Epinephrine acts via beta-adrenoceptor mechanisms to increase adenylate cyclase activity to form the second messenger cAMP that has the following metabolic effects:

1.  increases plasma glucose by breakdown of liver glycogen

2.  inhibits synthesis of glycogen

3.  stimulates gluconeogenesis

4.  breaks down fat (triglycerides) to fatty acids

salmeterol

1.  type

2.  uses

1.  beta adrenoceptor agonist

2.  treat bronchial asthma

What are the catecholamine reuptake inhibitors?

What are their major implications?

Cocaine and Tricyclic Antidepressants are the reuptake inhibitors. 

These inhibitors can be a problem if you administer them with other drugs that need to get into the nerve terminal to act.  If you block the channel, you can't get NE or any of the other drugs in.  Some of those drugs are:

1.  tyramine

2.  guanethidine

3.  6-OH dopamine