Attempt to consolidate info – there may be some drugs listed that we do not need to know.

Norepinepherine
(the sympathetic neurotransmitter) its effect in on the B₁, B₃ or the Alpha_1&2 receptors only….. no effect on lung B₂ receptors, only epinephrine effects B₂.

- drugs trying to block B₁ often effect B₂ as well leading to decreased resistence to Lido w/ epi – may get uncontrolled vasoconst. By epi mediated Alpha₁ activation

Review fig 10-3 for effect of blockers on vasodilation.

Drugs effecting Parasympathetic nervous system

Parasympathoimetic

See Musc. receptor Agonist

Methacholine, *carbachol, bethanechol

Anticholinesterase

(NO drugs effect Ach synthesis)

Tx of Myasthenia Gravis

Nerve Gas

Causes Bronchochonstriction and increased salivary flow

*Neostygmine

also Physostigmine

- Cognex and Aricept for alzheimers (in Alzheimers there is a relative deficiency of Ach .

Urinary incontinence

• Anticholinesterase

Oxybutaline

Cholinomimetic

Mimics parasymp. Stimulation but is not related to acteylcholine

Muscarinic Receptor Agonist

To combat cronic xyrostomia (only when glands are still functional)

Contraindicated

• Asthmaics

• COPD

• Some pts with cardiac conditions

• Causes abdominal cramps, myosis, renal colic

• Retinal detachment

• Chronic bronchitis

Pilocarpine (salagen)

M3 (W/ some M2) specific

Muscarinic Receptor Agonist

A more specific anti-xerostomia drug

• Particularly for sjogren’s syndrome

• Typical parasymp. Side effects (similar to above)

• Metabolized by P450 syst.

- Increased activity with p450 inhibitor drugs

• Effects offset by Anticholinergic drugs like benedril

Cevimaline

Cholinergic Agonist

Parasympatholitic

Inhibits parasympathetic

Anticholinergic

Centrally acting Anticholinergic

-Tertiary amine – for Tx of Parkinsons Dis. To counteract side effects of neuroleptic drugs on extrapyramidal syst.

-Contraindicated in Glaucoma myasthenia gravis, and obstructive GI dis.

-causes Xerostomia drowsiness and blurred vision.

Benzotropine (Cogentin)

Trihexphenidyl (Artane)

Anticholinergic

Antispasmodic Anticholinergic

• For Tx of GI disorders, peptic ulcers, hyperosmolarity

• Block smooth m. contraction but not in arteries, veins and bronchii (no B₂ action)

• Blocks abdominal cramps yet causes xyrostomia, and myosis

Glycopyrrolate (Robinol

Proprantheline (Pro-Bantheline) (anticholinesterase)

- now used primarily for anti-sialagogue

- H2 blockers now used for peptic ulcers

Acetylcholine storage depletion drugs

Inhibition of Acetylcholine acculumulation

Hemicholinium

Muscarinic receptor Antagonist

Blocks activity of ACH (Compet. Only??)

- used to combat cholinergic crisis

Atropine (also a belladonna alkaloid)

Belladona Alkaloid

(beautiful Lady)

Similar to above but must be able to penetrate CNS (Tertiary Amine)

Scopalamine (non-selective musc antagonist for motion sickness)

Nicotinic ganglionic Blocker

For Tx of malignant HTN

Trimethaphan

COPD (Anticholinergic Bronchodilator)

• B2 agonist are given for bronchodilation

• However Since musc. Receptors cause constriction Atrovent an anticholinergic drug is given to cause dilation. Better for COPD then B2 agonist

• precaution for use with BPH, glaucoma, bladder neck obstr.

• Inhaled – rinse mouth out after use to avoid unnecessary xerostomia.

Atrovent (also used for rhinorrhea

Drugs effecting the Sypathetic Nervous system

Mao Inhibitor

Epi will not break down as fast!!!

Enz breaks down Norepi. Collected by Uptake₁ into presynaptic Nerve Terminal.

• Avoid tyramine rich foods

• Not to be used with 5-HT drugs

Pargyline (MAO-A)

Selegine (MAO-B)

-some breaks do to amphetamine

COMT Inhibitor

Enz. breaks down Norepi taken up by Uptake₂ into the postsynaptic nerve terminal

• COMT inhibitors can be taken with parkinsons dis drugs to increase the ½ life of the drugs (levadopa)

Pyrogallol

Beta-Blocker

Non-Selective Beta Blocker

B₁ and B₂

- Tx of HTN, also pheocromocytoma,ezzential tremor, arrhythmias, MI, and open-angle glaucoma.

Do not use with Asthmatics – bronchospasms also not with cardiac pts, hypotentension, sinus bradycardia

- Must be carefull with Epi in lidocain, it will cause uncontrolled vasoconstriction by Alpha₁ Activity, and no response to B2 bronchodialators

Propranolol*, nadolol, timolol

B₁ blocker

Cardioselective beta-blocker

Selective for Heart- decreases contraction and rate

Does not effect B₂ in lungs

Metoprolol*

Atenolol*

(hepatic metabolism)

Alpha blockers (non-selective)

For enlarged prostate

Antagonizes (competitively) the effect of norepinepherine. Leads to prevention of vasoconstriction.

Phentolamine

Alpha₁ blocker

Will cause dilation of arterioles

For Tx of HTN

Also For enlarged prostate

*Prazosin, terazosin, dexazosin.

Alpha₁ Beta₁ blocker

Does not effect B₂ much (still a little), good idea but not very effective clinically and has many side effects

Labetolol

Alpha₁ Beta₁ Agonist

In the sense of neurotransmitter Norepi. Is the only one.

Norepinepherine

Adrenergic receptor agonist

Norepinepherine

B₂ Bronchodilator

B₂ Agonist (what is systemic skeletal M. effect??)

Used to treat asthma and COPD (anticholin. More effective for COPD - see below). Will still have some B₁ effect.

-Usually inhaled

Terbutaline*, Metaproterenol*

Albuterol, salmeterol, salbuterol

B₁ Agonist

Cardiolselective – increase CO, contractility, and rate

- also used in acute shock situations with failure of pump – leads to sympathetic jump start of myocardium

Dobutamine (IV)

Alpha₁ Agonist

Major factor in control of vasc. Tone

-causes vasoconstriction

Phenylepherine (in OTC cold meds), methoxamine

Centrally acting Alpha₂ Agonist

HTN drug

Pre-synaptic Alpha₂ in hypothalamus for control of sympathetic outflow to heart and blood vessel.

-Stimulation leads to sympathetic traffic. heart rate and CO, and peripheral vasodilation.

-Not used anymore due to severe xyrostomia leads to poor pt. Compliance

Clonidine

Alpha-NME

peripherally actingAlpha₂ Antagonist

Must be a tertiary amine in order to get into CNS. Increases male erectile efficiency.

Yohimbine (only one)

Uptake₁ inhibitor

In presynaptic membrane

Increased neurotransmission of Adrenergic sign(sympathetic storm)

Cocain, impramine

Indirect acting sympathomimetic

Amphedimine, ephedrine, tyramine.

Beta adrenergic Agonist?

Both B₁ and B₂ no alpha effect

Theraputic use is for Bronchodilation, but the major problem is tachycardia due to B₁ stimulation. Thus now an obsolete drug.

isoproterenol

Antiadrenergic

In emergency kits only for Tx of malignant HTN which will lead to MI or stroke.

Bretylium, guanathidine

Norepinepherine storage depleating drugs

Catecholamine delpletion based on inhibited uptake and storage. Used to be used for Tx of HTN

Reserpine