Lodge 2 Flashcards by Dakota Miller

Drugs: Prazosin, terazosin, doxazosin, tamsulosin, and alfuzosin

Alpha blockers

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Responses to Alpha blockers

Vasodilation (blood vessels of the skin, viscera, mucous membranes)

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Uses for Alpha blockers

Hypertension

* Benign Prostatic Hyperplasia (enlarged prostate)

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a1 Adrenergic Antagonists – Hypertension

a1-adrenergic antagonists relax smooth

muscle and decrease TPR.

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a1 Adrenergic Antagonists – BPH

•Tamsulosin(Flomax): a1-adrenergic antagonists relax smooth muscle in the prostate and bladder neck decreasing the degree of blockage of urine flow (treat symptoms).
• Side effects:
- dizziness when standing (due to vasodilation).
- inhibits ejaculation or causes retrograde ejaculation

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Side effects of directly-acting antagonists: the alpha blockers

Orthostatic hypotension
Tachycardia
Vertigo
Sexual dysfunction

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Uses for B blockers

tx of hypertension, ischemic heart disease, congestive heart failure, and certain arrhythmias

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Uses for Propranolol – prototypic non selective b Blocker

Hypertension
Migraine
Hyperthyroidism
Angina pectoris
Myocardial infarction

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Side effects of directly-acting antagonists: propranolol – prototypic non selective b Blocker

Fatigue
Bronchoconstriction
Sexual dysfunction
Arrhythmias

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Acetylcholine is released from parasympathetic postganglionic neurons as well as ALL _______ neurons

preganglionic & somatic

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Acetylcholine Synthesis occurs in nerve terminal and ______ is the rate limiting step.

Choline uptake

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Acetylcholine Inactivation

Hydrolyzed by acetylcholinesterase (AChE) in the synaptic cleft to form choline
Recycled
Terminated by pseudocholinesterase, widely distributed throughout the plasma

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Atony of the bladder
Atony of the GI tract
Myasthenia gravis (↓ muscle tone) - Intoxication by Ach antagonists
Glaucoma
Alzheimer’s Disease

Therapeutic uses of AChE inhibitors

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Reversible AChE Inhibitors include…

Physostigmine

- Neostigmine

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AChE Inhibitors can be used to treat _______ by increasing synaptic ACh.

Myasthenia Gravis

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______ is a nicotinic agonist that is NOT degraded by Acetyl cholinesterase

Suxamethonium

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______ (short duration AChE inhibitor) used to distinguish between “myasthenic” and “cholinergic” crisis in patients

Edrophonium

AChE Inhibitors can be used to treat _____ by restoring loss of function and not altering progression of the disease.

Alzheimer’s Disease

Tacrine, donepezil, rivastigmine, and galantamine

AChE inhibitors

Cholinergic Receptors:

agonist
as many as 12 sub-types
ligand-activated cation channels

Nicotinic

Cholinergic Receptors:

agonist
5 sub-types
G-protein coupled (7-TM)

Muscaranic

_______ are the principle cholinergic receptor in skeletal muscle and autonomic ganglia (BOTH sympathetic and parasympathetic) and are ligand-gated cation channels

Nicotinic receptors

Full agonist at Nicotinic Receptors and has both central and peripheral effects

Nicotine

• CNS stimulant 
- Arousal
- Increases mental performance
• Rewarding (activates DA system)
• Addictive

Nicotine Effects (central)

- Sympathomimetic (Increase BP and Heart Rate) | - Nicotine stimulates nicotinic receptors on adrenal medulla leading to epinephrine release

Nicotine Effects (periphery)

– A partial agonist at central a4b2-nicotinic receptor | – Possesses 50% of the intrinsic activity of nicotine – Prevents the binding of nicotine

varenicline (Chantix)

______ are the principle cholinergic receptor at autonomic ganglia (BOTH sympathetic and parasympathetic)

Nicotinic receptors

Because ganglonic antagonists block ______ function, the effect of these drugs depends upon the dominant tone in the organ system.

BOTH parasympathetic and sympathetic

Nicotinic Receptor Drugs: no longer of use for regulating autonomic functions (non specific)

NN (Ganglion)

Nicotinic Receptor Drugs: effects at muscles useful for paralysis during surgery

NM (NMJ)

Nicotinic Receptor Drugs: Smoking cessation, also promising advances with SELECTIVE ligands (i.e. Analgesia, Alzheimer's, schizophrenia)

NN (Brain)

Muscarinic receptors are localized to ________.

parasympathetic effectors

________ are the principle cholinergic receptor in smooth muscle, cardiac muscle and glands.

Muscarinic receptors

Muscarinic Agonist examples

- Bethanechol (non-selective) - Cevimeline (M3) - Atropine (non-selective) - Ipratropium/tiotropium (M)

Use of Cevimeline

* Muscarinic agonist (mainly M3) * Parasympathetic stimulation increases salivation * Used in dentistry to treat severe Xerostomia (dry mouth)

Side effects of Cevimeline

sweating, urination, stuffy nose, lacrimation, and abdominal pain

Use of Atropine

Decrease respiratory secretions as an adjunct for anesthesia

Effects of Atropine

* **Secretion **– Potently inhibits glandular secretion –particularly salivation (can be used in dental setting) * Eye – Persistent mydriasis (dilation) lasts 7-14 days * GI – Can be used as anti-spasmodic to reduce GI motility. * Urinary – reduce hyper-motility states of the urinary bladder, occasionally used in children. * Cardiovascular – Bimodal. Low doses inhibit presynaptic M1 receptors and increase Ach leading to bradycardia. High doses block M2 in SA node and increases heart rate.

Use and effects of Ipratropium/ tiotropium

* Used as second-line therapy for asthma (first line Albuterol– b agonist) * Therapeutic effects are specific due to inhalational application

_________ (i.e. Cevimeline) will stimulate salivation, however due to their side effects, muscarinic agonists are not widely used to treat this condition as there are satisfactory masticatory stimulants and artificial saliva products available OTC.

Muscarinic agonists

Patients taking parasympathomimetics (e.g., post-operative GI problems or glaucoma) should never be treated with _______ to reduce the flow of saliva.

anti-cholinergic drugs