Term
| Medulla Oblongata regulates what? |
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Definition
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Term
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Definition
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Term
| Hypothalamus regulates what? |
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Definition
| Temperature and osmolarity |
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Term
| What is the postganglionic sympathetic neurotransmitters? |
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Definition
NE (alpha, beta)
Neuropeptide Y, ATP |
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Term
| What is the preganglionic sympathetic neurtotransmitters? |
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Definition
Acetylcholine (nicotinic)
Enkephalin, Substance P, GnRH |
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Term
| What are the 5 diff. muscarinic "metabotropic" receptors and what type of receptors are they? |
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Definition
M1, M2, M3, M4, M5
Are G-Protein coupled receptors |
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Term
| What physiological/organs are affected when the 5 types of muscarinic receptors are activated? |
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Definition
M1: CNS, Autonomic ganglia, ***Parietal Cell***
M2: ***Cardiac***, SA & AV node, Autonomic ganglia
M3: ***Smooth Muscle Contraction***, Gland secretions, sweat, vasodilation
M4 and M5: CNS |
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Term
| What do the drugs Hemicholinium and Vesamicol do? |
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Definition
They have no clinical use
Hemicholinium: prevents choline re-uptake
Vesamicol: prevents vesicular storage of ACh |
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Term
| What does botulinum toxin do? |
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Definition
Degrades synaptobrevin (SNARE) and prevents vesicle fusion/exocytosis
Used clinically in cases with increased skeletal muscle tone, LES tone, focal dystonia |
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Term
| What does AChE inhibitors do? |
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Definition
| Elevates synaptic conc. of Ach and so increases postsynaptic effects of Ach. (parasympathomimetics) |
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Term
| What are 3 classes of anticholinesterases? |
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Definition
| Simple alcohols, carbamic acid derivatives, organophosphates |
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Term
| What does Edrophonium (simple alcohol) do? |
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Definition
| Has a short duration of action. Useful for diagnosing Myasthenia gravis and Eaton Lambert. |
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Term
| What do Neostigmine and Physostigmine do? (Carbamic acid derivatives) |
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Definition
| Longer duration of action. Useful for treating MG. Reversal of neuromuscular blockers. |
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Term
| What does Isofluorophate (organophosphate) do? |
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Definition
It is irreversible and toxic.
Commonly used in flea/tick meds. |
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Term
| What are 4 uses of acetylcholine esterase inhibitors? |
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Definition
1) Used to increase neuromuscular transmission (skeletal)
2) Increase parasympathetic tone (parasympathomimetic)
3) Increase central cholinergic neurotransmission in dementia
4) Reversal of paralysis from non-depolarizing neuromuscular blockers |
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Term
| How do muscarinic receptor agonists benefit the eye, GIT/bladder/urinary tract, and salivary glands? |
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Definition
Eye: Contracts smooth muscle, decreases intraocular pressure, and benefits glaucoma
GIT/Bladder/Urinary Tract: Contracts smooth muscle so restores GIT and UT motility after anesthesia/surgery
Salivary Glands: Increases salivation so benefits xerostomia |
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Term
| Why is Ach not used clinically? |
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Definition
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Term
| What are 3 muscarinic receptor agonists? |
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Definition
| Carbahol, pilocarpine, and Methacholine (used in diagnosis of asthma) |
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Term
| How do muscarinic receptor antagonists ("parasympatholytics") work and an example drug? |
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Definition
They bind to muscarinic receptors and prevent Ach from exerting its effects.
Ex: is Atropine. It causes pupil dilation, tachycardia, decreased secretions |
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Term
| What are 4 uses of Atropine? |
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Definition
1)To produce mydriasis for opthalmological examination (applied topically)
2)To reverse sinus bradycardia caused by excessive vagal tone
3)To inhibit excessive salivation and mucus secretion during anesthesia and surgery
4)To counteract the effects of muscarine poisoining AND poisoining with anticholinesterases |
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Term
| Other than Atropine, name 3 other muscarinic antagoninsts used clinically |
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Definition
1)Scopolamine: Significant CNS effect
2)Pirenzepine: Treatment of peptic ulcers
3)Ipratropium: Relatively selective for M3, reduces bronchial secretions-used in COPD, used in asthma |
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Term
| What is a drug that is a nicotinic receptor agonist? |
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Definition
Succinylcholine: depolarizing neuromuscular blocker
Used in short term paralysis, during intubation. Has short duration as metabolized by pseudocholinesterases (BuChE)
Side effects are bradycardia, K+ release, prolinged paralysis, malignant hyperthermia |
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Term
| What do nicotinic receptor antagonists (non-depolarizing neuromuscular blockers) do and what is their mode of action? |
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Definition
Used to paralyze skeletal muscles during surgery
Mode of action is to occupy the Nm receptors on skeletal muscle, prevent action of Ach, muscle cannot contract so flaccid paralysis |
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Term
| Some example drugs which are nicotinic receptor antagonists (non-depolarizing neuromuscular blockers)? |
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Definition
D-tubocurarine: Plant alkaloid ("arrow poison")
Pancuronium: Long-acting
Vecuronium: Intermediate
Mivacurium: Short-acting
These are more selective on Nm rec than Nn rec (ganglia) |
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Term
| All cathecholamines are synthesized from what neurotransmitter? |
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Definition
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Term
| What are the 5 types of adrenergic receptors and what do they do? |
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Definition
Alpha 1: Increase IP3/DAG, Increase Ca2+ and PKC
Alpha 2: Decrease cAMP, Increase K+ and decrease Ca2+
Beta 1: Increase cAMP, Increase PKA
Beta 2: Increase cAMP, Increase PKA
Beta 3: Increase cAMP, Increase PKA |
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Term
| All adrenergic receptors are linked to what? |
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Definition
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Term
What are the post-synaptic physiological effects of alpha-1 adrenergic receptor?
Or What is effect of NE on alpha-1 adrenergic receptor? |
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Definition
Smooth muscle contraction
Vasoconstriction
Pupil dilation
Ejaculation |
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Term
What are the pre and post-synaptic physiological effects of alpha-2 adrenergic receptor?
Or What is effect of NE on alpha-2 adrenergic receptor? |
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Definition
Presynaptic: Decrease NE release
Postsynaptic: Decrease insulin release |
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Term
| Or What is effect of NE on Beta-1 adrenergic receptor |
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Definition
Increase contractility of heart and HR
Increase renin secretion and that causes other things like increses in: vasoconstriction and TPR, and aldosterone and blood volume |
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Term
| Or What is effect of NE on Beta-2 adrenergic receptor |
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Definition
Smooth muscle relaxation (bronchodilation and uterine relaxation)
Metabolic effects: Increases in: lipolysis, glucagon, liver glucose production |
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Term
| What are some overall effects of NE on metabolism? |
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Definition
Increase blood glucose
Increase availability of energy |
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Term
| What happens if Beta-3 adrenergic receptor gets activated? |
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Definition
| Lipolysis of adipose tissue |
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Term
| Epi. has higher affinity for Alpha or Beta adrenoreceptors? |
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Definition
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Term
Epi. at high concentrations has effects on what?
At high doses it is good at treating what? |
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Definition
At higher conc., it has an effect on alpha-1 adrenoreceptors
At high doses, it is effective at treating anaphylaxis and used for vasoconstriction in conjunction with local anesthetic |
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Term
Norepi. has greater affinity for what adrenoreceptors?
Has little affinity for? |
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Definition
Greater affinity for alpha-1 and Beta-1 adrenoceptors.
Has little affinity for Beta-2 adrenoceptors. |
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Term
| Example of an alpha-1 agonist drug and its effect? |
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Definition
Phenylephrine
Used as nasal decongestant. Also used for treatment of shock.
Side-effect: HTN |
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Term
| Example of alpha-1 antagonist drugs and their effects? |
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Definition
Prazosin: Used for HTN and Benign Prostatic Hypertrophy
Side effects: Postural orthostatic / hypotension related to 1st dose phenomenah
Tamsulosin: Used for Benign Prostatic Hypertension. More selective for genitourinary smooth muscle receptor subtype. Less postural / orthostatic hypotension |
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Term
| Example of an alpha-2 agonist drug and its effect? |
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Definition
Clonidine: Used for rx of HTN and opioid withdrawal
Side effects: Bradycardia & HTN |
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Term
| Example of an alpha-2 antagonist drug and its effect? |
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Definition
Yohimbine: previously used for male impotence
Side effects: HTN |
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Term
| Example of a non-selective Beta receptor agonist drug and its effect? |
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Definition
Isoproterenol: Used for emergency arrhythmias & bronchospasm. More selective agonists now available.
Side effects: HTN, palpitations, tremor |
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Term
| Example of selective Beta-1 agonist drug and its effect? |
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Definition
| Dobutamine: Has prominent inotropic effects resulting in increased contractility and CO. Used in acute HF. Short half-life due to COMT metabolism. |
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Term
| Examples of selective Beta-2 receptor agonist drugs their effects? |
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Definition
These types of drugs used for treatment of asthma
Albuterol: Asthma reliever. Rapid action, relative short duration
Salmeterol: Prevents bronchoconstriction. Long-acting Beta agonists. Have lipophilic side chains that resist degradation. |
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Term
| What do Beta-Adrenergic Antagonists do? |
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Definition
Block Beta-1 receptors so decrease chronotropic and ionotropic actions, and reduce renin secretion. Are first line drugs to treat HTN.
Blocking Beta-2 drugs is clinically undesirable. |
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Term
| What is one example of a non-selective Beta adrenoreceptor antagonist? |
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Definition
Propranolol: Used for HTN, angina
Side effects include sedation (central effect) and dyspnea. |
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Term
| Example of B1-Selective Adrenergic Antagonists? |
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Definition
Atenolol: HTN and angina. Used in rx of heart failure (decreases renin production so decreases volume reduction). **Contraindicated in severe HF**
Side effects is similar to Propanolol but less severe. |
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Term
| What are partial Beta-1 Selective Adrenergic Antagonists used for? |
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Definition
| Reduces effect of endogenous NE at Beta-1 receptors so this leads to smaller decreases in resting HR and BP (compared to Beta-1 receptor antagonists). |
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Term
| Example of a Partial Beta-1 agonist and its use? |
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Definition
| Pindolol: Clinically used for treatment of HTN in patients with bradycardia or low cardiac reserve |
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Term
| Example of a nonselective Beta and Alpha-Antagonist? |
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Definition
| Carvedilol: Alpha-receptor blockade results in vasodilation. Beta-1 blockade prevents a reflex sympathetic increase in HR. Both effects combine to decrease BP. Used in treatment of HF. **Contraindicated in severe HF** |
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Term
| COMT (Catechol-O-methyl transferase) is primarily expressed where? |
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Definition
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Term
| What are 3 drugs that are inhibitors for re-uptake? |
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Definition
Cocaine: Inhibits NET
Tricyclic Antidepressants (TCAs): Inhibit NET
Imipramine: Treats mild depression
Side Effects: Postural hypotension and tachycardia |
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Term
| Two drugs that are inhibitors of storage? |
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Definition
Reserpine: Blocks VMAT
Tyramine: Transported via VMAT & displaces vesicular NE |
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Term
| 3 drugs that are inhibitors of metabolism? |
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Definition
MAO Inhibitors: Used for treatment of mild depression
Phenelzine: Non-selective MAO inhibitor. Implicated in elevated tyramine leading to hypertensive crisis
Selegiline: Selective MAO B inhibitor. Safer with respect to dietary restriction. Also used for Parkinson's |
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Term
| What three drugs are inhibitors of Re-Uptake and Storage? |
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Definition
1) Amphetamines
a)Displaces endogenous catecholamines from storage vesicles
b)blocks NET
c)a weak inhibitor of MAO
2)Methylphenidate: Used for ADHD
3)Ephedrine & Pseudoephedrine: Used for nasal decongestion |
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