PHARMA ANS

The central nervous system (CNS) is the body’s primary nervous system, consisting of the ___ and ___.

The peripheral nervous system (PNS), located outside the brain and spinal cord, is made up of two divisions:

Also called the visceral system, acts on smooth muscles and glands.

Its functions include control and regulation of the heart, respiratory system, gastrointestinal tract, bladder, eyes, and glands.

an involuntary nervous system over which we have little or no control.

is a voluntary system that innervates skeletal muscles, over which there is control.

Two set of neurons in autonomic component of PNS

send impulses to the CNS, where they are interpreted.

receive the impulses (information) from the brain and transmit these impulses through the spinal cord to the effector organ cells.

The efferent pathways in the ANS are divided into two branches

Also called the adrenergic system

is the neurotransmitter that innervates smooth muscles.

is released from the terminal nerve ending and
stimulates the cell receptors to produce response.

Adrenergic receptor organ cells are of four types:

The sympathetic and parasympathetic nervous systems act on the ___ organs but produce ___ responses to provide ___ (___)

Drugs that stimulate the sympathetic nervous system are called ___ ___ because they mimic the sympathetic neurotransmitters norepinephrine and epinephrine.

Increases force of heart contraction; vasoconstriction increases blood pressure; mydriasis (dilation of pupils) occurs; decreases secretion in salivary glands; increases urinary bladder relaxation and urinary sphincter contraction

Inhibits release of norepinephrine; dilates blood vessels; produces hypotension; decreases gastrointestinal motility and tone

Increases heart rate and force of contraction; increases renin secretion, which increases blood pressure

Dilates bronchioles; promotes gastrointestinal and uterine relaxation; promotes increase in blood sugar through glycogenolysis in liver;
increases blood flow in skeletal muscles

When these receptors in vascular tissues (vessels) of muscles are stimulated, the arterioles and venules constricts; this increase peripheral resistance and blood return to the heart, circulation improves, and blood pressure is increased. When too much stimulation occurs, blood flow decreased to the vital organs.

These receptors are in the postganglionic sympathetic nerve endings, when stimulated, they inhibit the release of norepinephrine, which leads to a decrease in vasoconstriction. This results in vasodilation and a decrease in blood pressure.

Receptors are located primarily in the heart but are also found in the kidneys. Stimulation of this receptor increase myocardial contractility and heart rate

Receptors are found mostly in the smooth
muscle of the lung and GI tract, the liver, and
the uterine muscle.

These receptors:
1. Relaxation of the smooth muscles of the
lungs which results in bronchodilation
2. A decrease in GI tone and motility
3. Activation of glycogenolysis in the liver and
increase blood glucose.
4. Relaxation of the uterine muscles, which results in a decreased uterine contraction

Other adrenergic receptor is ___ and are located in the renal, mesenteric, coronary, and cerebral arteries. When these receptor are stimulated, the vessels dilate and blood flow increases.

Other adrenergic receptor is dopaminergic and are located in the renal, mesenteric, coronary, and cerebral arteries. When these receptor are stimulated, the vessels dilate and blood flow increases. Only ___ can activate this receptor.

Transmitters are inactivated by:

The two enzymes that inactivate norepinephrine are:

Classification of Sympathomimetics

which directly stimulate the adrenergic receptor (e.g., epinephrine or norepinephrine)

which stimulate the release of norepinephrine from the terminal nerve endings (e.g., amphetamine)

which stimulate the adrenergic receptor sites and stimulate the release of norepinephrine from the terminal nerve endings

is an example of a mixed-acting sympathomimetic.
This drug acts indirectly by stimulating the release of norepinephrine from the nerve terminals and acts directly on the alpha1 and beta1 receptors.
It increases heart rate. It is not as potent a vasoconstrictor as epinephrine, and there is less risk of hemorrhagic stroke and hypertensive crisis.

is helpful to relieve nasal and sinus congestion without rebound congestion.

are the chemical structures of a substance (either endogenous or synthetic) that can produce a sympathomimetic response.

From what category of catecholamines do these belong:
epinephrine, norepinephrine, and dopamine

From what category of catecholamines do these belong:
isoproterenol and dobutamine

stimulate the adrenergic receptors. Most of them have a longer duration of action than the endogenous or synthetic catecholamines.

(Adrenalin), which acts on alpha1-, beta1-, and beta2- adrenergic receptor sites. The responses from these receptor sites include increase in blood pressure, pupil dilation, increase in heart rate (tachycardia), and bronchodilation.

In anaphylactic shock, ___ is useful because it increase blood pressure, heart rate, and airflow through the lungs.

Because epinephrine affects different adrenergic receptors, it is ___.

a beta2-adrenergic agonist, is selective for beta2-adrenergic receptors, so the response is relaxation of bronchial smooth muscle and bronchodilation.

action is more selective (activates only the beta2 receptors). By using selective sympathomimetics, fewer undesired adverse effects will occur However, high dosages of this may affect beta1 receptors, causing an increase in heart rate.

✓ is a selective alpha2-adrenergic agonist (sympathomimetic) used primarily to treat hypertension.

✓ Alpha2 drugs act by decreasing the release of norepinephrine from sympathetic nerves and decreasing peripheral adrenergic receptor activation.

✓ Alpha2 drugs also produce vasodilation by stimulating alpha2 receptors in the central nervous system (CNS), leading to a decrease in blood pressure

✓ is an alpha-adrenergic agonist (sympathomimetic) that acts within the CNS.

✓This drug is taken up into the brainstem neurons and converted to methylnorepinephrine, which is an alpha2-adrenergic agonist that leads to alpha2 activation.

✓ The decrease of sympathetic outflow from the CNS causes vasodilation and a reduction in blood pressure

Drugs that block the effects of adrenergic neurotransmitters

They act as antagonists to adrenergic agonists by blocking the alpha and beta receptor sites.

Most adrenergic blockers block either the alpha
receptor or the beta receptor. They block the effects of the neurotransmitter either directly by occupying the receptors or indirectly by inhibiting the release of the neurotransmitters norepinephrine and epinephrine.

Drugs that block or inhibit a response at the alpha-adrenergic receptor site

Alpha-blocking agents are divided into two groups:

promote vasodilation, causing a decrease in blood pressure.

If vasodilation is long-standing, ___ ___ can result.

___ may also be a symptom of a drop in blood pressure.

As blood pressure decreases, pulse rate usually ___ to compensate for the low blood pressure and inadequate blood flow.

___ ___can be used to treat peripheral vascular disease (e.g., Raynaud’s disease).

These drugs are also helpful in decreasing symptoms of benign prostatic hyperplasia.

Commonly called beta blockers, decrease heart rate, and a decrease in blood pressure usually follows.

Some beta blockers are nonselective, blocking both beta1 and beta2 receptors. Not only does the heart rate decrease because of beta1 blocking, but ___ also occurs.

Nonselective beta blockers (block both beta1 and beta2) should be used with extreme caution in any patient who has ___ or ___.

was the first beta blocker prescribed to treat angina, cardiac dysrhythmias, hypertension, and heart failure.

This medication is given for migraine prophylaxis.

is the ability of certain beta blockers to bind with a beta receptor to prevent strong agonists from binding to that receptor producing complete activation.

The selective blocker (blocks beta1 only) that has ISA is ___

a selective Beta blocker, decreases sympathetic outflow to the periphery and suppresses the renin-angiotensin-aldosterone system (RAAS) response.

It is contraindicated in bradycardia, heart block, cardiogenic shock, acute heart failure, asthma, and sick sinus syndrome.

Beta-adrenergic Antagonists should not be abruptly discontinued but rather should be tapered off over __ to __ weeks to avoid tachycardia, HPN, severe angina, dysrhythmia and MI.

Atenolol has a half life of __ to __ hours and is eliminated in urine

The use od decongestants with epinephrine has an ___ effect.

___ can antagonize the action of epinephrine.

___ and ___ allow epinephrine effects to be intensified and prolonged.

For Atenolol, the onset of action of the oral preparation is __ hour; peak time is __ to __ hours, and duration of action is __ hours. This drug is effective for dosing __ a day, especially for patients who do not adhere to schedules that require dosing several times a day.

___decrease the hypotensive effect of atenolol.

When atenolol is given concurrently with ___ and other anticholinergics, absorption is increased.

Drugs that block the release of norepinephrine from the sympathetic terminal neurons, which are classified as a subdivision of the adrenergic blockers.

Two groups of drugs affect the parasympathetic nervous system they include:

muscarinic agonists or parasympathomimetics

(blocking agent)-muscarinic antagonists, parasympatholytic or commonly called anticholinergics.

The parasympathetic nervous system is called the ___ system because the neurotransmitter at the end of the neuron that innervates the muscle is ___.

The cholinergic receptors at organ cells are either ___ or ___,

Acetylcholine stimulates the receptor cells to produce a response, but the enzyme ___ may inactivate acetylcholine before it reaches the receptor cell.

Drugs that mimics the neurotransmitters norepinephrine and acetylcholine produce responses ___ to each other on the same organ.

Drugs that stimulates the PNS are called ___ ___, or ___, because they mimic the parasympathetic neurotransmitter acetylcholine.

The neurotransmitter located at the ganglions and the parasympathetic terminal nerve endings.
-it innervates cholinergic receptors on organs, tissues, and glands.

Two types of cholinergic receptors are

cholinergic receptor which stimulates the smooth muscles and slow the heart rate.

cholinergic receptor which affects the skeletal muscles.

The ___ bind the enzyme cholinesterase for several minutes to hours

___ bind the enzyme permanently.

are primarily selective to the muscarinic receptors but are nonspecific because the muscarinic receptors are located in the smooth muscle of the GI and genitourinary tracts,glands, and heart.

a direct-acting cholinergic agonist, acts on the muscarinic (cholinergic) receptor and is used primarily to increase micturition (urination) in the treatment of urinary retention and neurogenic bladder.

is a direct-acting cholinergic agonist that is usually prescribed to treat gastroesophageal reflux disease (GERD). It accelerates gastric emptying time.

is a direct-acting cholinergic agonist that constricts the pupils of the eyes, thus opening the canal of Schlemm to promote drainage of aqueous humor (fluid).

This drug is used to treat glaucoma by relieving fluid (intraocular) pressure in the eye and to promote miosis in eye surgery and examinations.

Drugs that inhibit the actions of acetylcholine by occupying the acetylcholine receptors are called

Was first derived from the belladonna plant (Atropa belladonna) and purified in 1831, is a classic anticholinergic, or muscarinic antagonist drug.

was the second belladonna alkaloid produced.

It is useful primarily
(1) as a preoperative medication to decrease salivary secretions and
(2) as an agent to increase heart rate when bradycardia is present.