Pharm Block 1-ANS

ptheodore's version from 2016-09-23 23:01

ANS Receptors

NameTypeEffector enzymeSecond MessengerProtein Type
M1Gqstimulate PLCincreased IP3 and DAGG-protein coupled
M3Gqstimulate PLCincreased IP3 and DAGG-protein coupled
α1Gqstimulate PLCincreased IP3 and DAGG-protein coupled
α2GiInhibit adenylyl cyclaseDecrease cAMPG-protein coupled
M2GiInhibit adenylyl cyclaseDecrease cAMPG-protein coupled
β1,2,3Gsstimulate adenylyl cyclaseIncrease cAMPG-protein coupled
NNm & Nnn/an/aIon channel receptor (Increases Na+ ion movement into cells)

Receptor Location & Function

Question Answer
M1Neurons, CNS Effects
M2Heart, Reduces heart rate…bradycardia
M3Smooth muscle and glands (Contraction (except in blood vessels)… diarrhea, bronchoconstriction, urination, ↑ Secretions ….salivation, stomach acid, sweating, lacrimation. Exocrine glands, ciliary musc. of eye). Pupil and ciliary muscle (Contracts ...Miosis, increased flow of aqueous humor )
NmSkeletal muscle end plate (Contraction of skeletal muscle)
NnGanglions. Stimulation of post gang fibres
α1Blood vessels Pupil (Iris) smooth muscle (Vasoconstriction, Mydriasis sphincter contraction…so Constipation and Urinary retention) & Prostate & Urinary Bladder
α2Presynaptic nerve terminals ( Reduces release of norepinephrine…bradycardia, hypotension)
β1Heart (Contraction, Increased heart rate). JGA, ↑ renin release
β2Smooth muscles ( Relaxation …so bronchodilation, urinary retention, constipation, uterus relaxation. Vascular smooth muscles), Skeletal Muscle (K+ uptake), Pancreatic Beta Cells (Insulin release)
β3Fat tissue (lipolysis)
D1Kidney's (dilates renal vessels). Activates Adenyl Cyclase. Smooth Muscles

Adrenergic Transmission

Question Answer
Affects synthesize of DOPA by blocking Tyrosine HydroxylaseMetyrosine
Affects the storage of NE & Dopamine (Side Effect: Cause Major DEPRESSION). Use for Hypertension. Affects VMAT.Reserpine
Affects the release of NE & Dopamine (Side Effect: Postural hypertension & reflect tachycardia)Bretylium & Guanethidiene
Inhibits Dopamine and Nor-epinephrine reuptakeCocaine & Tricyclic Antidepressants (TCA)

Cholinergic Transmission

Question Answer
Blocks uptake of AchHemicholiniums
Blocks storage of AchVesamicol
Blocks release of Ach by affecitng the SNAPS & VAMPSBotulism toxin

Cholinergic drugs

Question Answer
They act by binding directly to Cholinergic receptors (cholinoceptors)Bethanechol, Pilocarpine, Carbachol (Direct acting Cholinergic agonists)
Indirect IRREVERSIBLE cholinergic agonistsEcothiophate, Malathion, Parathion, Sarin (OrganoPhosphates)
Use in isecticidesMalathion, Parathion
Used as a Nerve GasSarin
Rx for Paralytic ileus: It is the condition characterised by reduced bowel movements, inability to pass stools or flatus. Typically seen in postoperative patients.Bethanechol
Rx for Urinary retention (Non obstructive): Typically seen in postoperative patients and many other neurological diseasesBethanechol
By stimulating M3 receptors ___increases the bowel movements and bladder contractionBethanechol
By stimulating M3 receptors ____increases the bowel movements and bladder contractionBethanechol
Rx for Glaucoma (due to increased intraocular tension): that constrict the pupils and increase draining of the aqueous humorPilocarpine
Rx for Sjogren's syndromePilocarpine
Irreversible Indirect acting Cholinergic agonists used to treat glaucomaEcothiopate
A tertiary amine, lipid soluble. Therefore used in glaucoma treatment~Physostigmine
Mechanism for PhysostigmineReversible inhibition of AChE enzyme- ↑ Ach. It helps by causing miosis- ↑ outflow of aqueous humor- ↓ IOP
Reversible Acetyl Cholinesterase inhibitors used to treat Myasthenia gravisNeostigmine, Pyridostigmine
Has a longer duration of action. So good for maintenance/long term therapy of M. Gravis. Given orally.Pyridostigmine
Used in acute cases of M. Gravis. Given I. V.Neostigmine
Reversible Acetyl Cholinesterase inhibitor used to diagnose Myasthenia gravis (Tensilon test)Edrophonium
The shortest acting for 5 minutes~. So used in diagnosis of M. Gravis and to differentiate myasthenic and cholinergic crisis by doing a Tensilon testEdrophonium
Indirect Reversible Acetyl cholinesterase inhibitors used to treat Alzheimer’sTacrine, Rivastigmine and Donepezil
Organophosphorous compounds (OP).Ecothiopate, Malathion, Parathion & Sarin
Organophosphorus compounds are irreversible cholinesterase inhibitors. Signs and symptoms are due to ____ (irreversible inhibition) of the enzyme resulting in excess acetylcholinePhosphorylation
1st concern of organophosphate poison is dealing with theBronchoconstriction
A muscarinic receptor blocker (Anticholinergic drug), is given to control signs of muscarinic excess stimulation of OP compoundsAtropine
This is a Acetylcholine esterase reactivator. This acts by hydrolysing (reactivating) the drug bound enzyme, this should be given as early as possible, before “Aging” of the enzyme during OP poisoning.Pralidoxime (2-PAM)
What type of drugs contrict pupils and increase draining of the aqueous humorMiotics (Rx; glaucoma)
Indirect cholinergic agonists act by ____ “Acetyl cholinesterase” the enzyme required for metabolism of ACh in synapase. Thus increases Acetylcholine level in synapses.Inhibiting
Reverses the central and peripheral signs of muscarinic blockade (Atropine Poising)Physostigmine

Anticholinergic drugs (M Blockers)

Question Answer
Used To treat Cholinesterase inhibitors / Organophosphate (OP) pesticides poisoningAtropine
Shortest acting preparation of AtropineTropicamide
Rx for Peptic UlcersPirenzepine
Rx for motion sicknessScopolamine
Used to treat drug induce Parkinson (Extrapyramidal symptoms)Benztropine
Used ONLY in asthma/COPDIpratropium Bromide
Rx for GI Pain and Menstrual crampsDicyclomine
Reverses the central and peripheral signs of muscarinic blockade (Atropine Poising)Physostigmine
Acts for 4 hours, is preferred to produce mydriasis and cycloplegia (paralysis of the ciliary muscle of the eye, resulting in a loss of accommodation (side effect)) in refraction error testing and fundoscopyTropicamide
Nicotinic receptors (Nn) or ganglionic blockersHexamethonium, Mecamylamine
Side effect of Hexamethonium, MecamylamineSevere Hypotension

Adrenergic Recptors & Drugs

Question Answer
Adrenergic Receptors in Prostate & Urinary Bladderα1
Adrenergic Receptors in Presynaptic nerve terminals (Inhibition of transmitter release- ↓ sympathetic outflow)α2
Adrenergic Receptors in Heart (Contraction, Increased heart rate). JGA, ↑ renin releaseβ1
Adrenergic Receptors in Skeletal Muscle (K+ uptake), Pancreatic Beta Cells (Insulin release)β2
Adrenergic Receptors in Pancreatic Beta Cells (Insulin release)β2
Adrenergic Receptors in Fat tissue (lipolysis)β3
Adrenergic Receptors in Kidney's (dilates renal vessels). Activates Adenyl Cyclase. Smooth MusclesD1
Drug involve in displacement of stored catecholamines from the adrenergic nerve endingAmphetamine, methamphetamine and Tyramine
Drug involve in Inhibition of reuptake of catecholamine’s already releasedCocaine & Tricyclic antidepressants

Adrenergic Recptors & Drugs

Clonidine α2
Isoproterenolβ1, β2
Norepinephrineα1, β1, β2
Epinephrineα1, α2, β1, β2
Dopamine D1, D2
Low Dose of Dopamine activatesD1
Moderate Dose of Dopamine activatesβ1
High Dose of Dopamine activatesα1
Used as mydriatic for retinoscopy (NO cycloplegia) Phenylephrine
α2 selective agonists can be used in treatment of glaucomaApraclonidine, Brimonidine
β antagonists decrease the production of aqueous humor- hence can be used in treatment of glaucomaTimolol
At low epinephrine concentrations, the ___receptors will be occupied because these receptors have a higher affinity of epinephrine β2
At high epinephrine concentrations, the ___receptors will be occupied because there are more of these receptors the predominant effect at high concentrations is vascular smooth muscle contraction. α1
Epi is combined with to reduce the systemic absorption of anesthetic, and increase their duration of actionLidocaine (local anesthetic)
Nasal decongestant to reduce the discomfort of hay fever & the common coldPhenylephrine
Use for Short term hypotensive emergencyPhenylephrine
These drugs are used as topical decongestants because of their ability to promote constriction of the nasal mucosa.Xylometazoline and oxymetazoline
Use for HT in pregnancy (Pre-eclampsia)Clonidine & alpha methyldopa
Side effects: Postural hypotension, dry mouth, sedation, rebound hypertensionClonidine & alpha methyldopa
A clonidine derivative used in glaucomaApraclonidine, Brimonidine
To produce bronchodilation in treatment of Bronchial asthma and COPD.Albuterol, terbutaline, Salmeterol
Rx for Premature labor, threatened abortionAlbuterol, terbutaline, Salmeterol
Increases the release of monoamines (norepinephrine & dopamine) from their storage sites.Amphetamine
Important chiefly because of its use and misuse as a CNS stimulant. It has marked stimulant effects on mood and alertness and a depressant effect on appetite.Amphetamine
A new amphetamine substitute, used in narcolepsy and is claimed to have fewer adverse effectsModafinil
Rx for Attention-deficit hyperactivity disorder (ADHD) Methylphenidate
Inhibition of transmitter reuptake at noradrenergic synapses.Cocaine
Tachyphylaxis developsEphedrine
If taken orally while taking MAO inhibitors (antidepressants), it produces effects similar to norepinephrine, and can possibly cause a hypertensive crisisTyramine



Question Answer
Irreversible non selective alpha 1&2 blocker, insurmountable blockade of alpha receptors, forms covalent bond with receptorsPhenoxybenzamine
Use to treat Pheochromocytoma & HTPhenoxybenzamine
Reversible non-selective alpha 1 & 2 blockerPhentolamine
Selective alpha 1 & 2 blocker use for treatment of ESSENTIAL HTNPrazosin
Selective alpha 1& 2 blockers arePrazosin, Terazosin, doxazosin
An alpha 1 selective blocker use to treat prostate and urinary bladder abnormalitiesTamsulosin
A reversible selective alpha-1 blockerYohimbine
In terms of drugs combination what is a competitive antagonistcombination dose curve of two drugs
What is a partial agonistalways a dose curve of a single drug
Type of blockers that can lead to orthostatic hypertension, and reflex tachycardia, epinephrine reversalalpha blockers
What type of blockers are approved for use in men with urinary symptoms due to benign prostatic hyperplasia (BPH)alpha blockers
Use to treat essential HTNPrazosin
Use to treat HTN due to clonidine withdrawal, cheese reactionphentolamine
Calcium channel blockers are preferred drugs use to treat peripheral vascular disease such Raynaud's phenomenon. What is another alternative alpha blocker can be used to treat PVD?Prazosin
Selective alpha 1a blockerTamsulosin and Terazosin
Use to treat Benign Prostatic Hyperplasia (BPH) & HTNPrazosin
Which drug can be used to reduce prostate hyperplasia & reverse prostate hypertrophy?Fenesteride
What is the standard treatment for Pheochromocytoma?Phenoxybenzamine plus beta blocker
Toxicity of alpha blockers can lead toOrthostatic hypotension aka postural hypotension, reflex tachycardia
What type of blockers need to be used to treat a patient with HTN and bronchial asthma?Selective beta blocker
Name the non-selective beta blockersNadolol, propranolol, timolol, Labetalol and carvedilol
What are the two non-selective beta blockers that are also considered alpha blockers?Labetalol & Carvedilol
Name the selective beta blockersAtenolol, Betaxolol, Esmololo, Acebutalol, Metoprolol
Name a selective beta blocker that has shortest half-life and used in surgery for short term control of cardiac arrhythmiaEsmolol
Name the two partial agonist of beta-1-selective block use to treat asthmaPindolol & acebutolol
Why partial agonist drugs are favorable to treat asthma?Because they are less likely to cause bronchospasm
Which type of beta adrenergic drug use as a local anesthetic to block sodium channelPropranolol
What is the disadvantage of using propranolol in the eye?Decrease protective reflex of the eye & increase corneal ulceration
Beta-1 blockers specially Atenolol are safe to treatAsthma
What are the effect and clinical use of beta blockers?decrease cardiac output, decrease renin secretion
Drug use to teat cardiac arrhythmiasSotalol
Drug use to treat heart failureCarvedilol, Metoprolol, bisoprolol
Drug use to treat glaucomaTimolol
Drug use to treat pheochromocytomaLabetalol
Drug use to treat migraine headache and performance anxietyPropranolol
Which drug use to treat heart failure but also useful for long term remodeling of the heart?Carvidilol
What are the majors side effect of the use of beta blockers?Bronchospasm, bradycardia