Pharmacology - Block 1 - Part 3

davidwurbel7's version from 2016-08-14 05:23


Question Answer
Nicotinic Receptors present on the skeletal muscleN[M]
Nicotinic receptors present on the ganglionic neurons and in the brain medullaN[N]
Muscarinic receptor present in cardiac muscleM2
Muscarinic receptor present everywhere except the cardiac muscleM3
Alpha adrenergic receptors present on pre-synaptic neurons that autoregulate release of neurotransmitterAlpha 2
Alpha adrenergic receptors present in blood vessels, pupil and smooth muscleAlpha 1
Beta adrenergic receptors present in the heartBeta 1
Beta adrenergic receptors present in the smooth musclesBeta 2
Beta adrenergic receptors present in adipose tissueBeta 3
The type of receptors present in the renal tubularDopaminergic
Beta 1, 2, 3 receptors use this G-coupled proteinGs
M1, M3, alpha 1 receptors use this G-coupled proteinGq
M2 and alpha 2 receptors use this G-coupled proteinGi


Question Answer
The effect of this neurotransmitter on the heart M2 receptors is a decrease in HR, FOC, and COAcetylcholine
The effect of this neurotransmitter on the blood vessels M3 receptors is the production of nitric oxide causing vasodilation and low blood pressureAcetylcholine
The effect of this neurotransmitter on the smooth muscle M3 receptors is contraction….bronchospasm, diarrhea, urination and relaxation of the sphincters except the lower esophageal sphinctersAcetylcholine
The effect of this neurotransmitter on the pupil M3 receptors causing miosis, ciliary muscle contraction, increase in lens curvature, eye is fixed for near vision, cyclospasm, increase aqueous humor drainageAcetylcholine
The effect of this neurotransmitter on glands M3 receptor causes secretionAcetylcholine
The effect of this neurotransmitter on the heart beta 1 receptors is an increase in HR, FOC, and CONorepinephrine
The effect of this neurotransmitter on the blood vessels beta 2 receptors causes vasoconstriction and an increase in blood pressureNorepinephrine
The effect of this neurotransmitter on the smooth muscle beta 2 receptors causes relaxation - bronchodilation, constipation, urinary retention and contraction of the sphincters Norepinephrine
The effect of this neurotransmitter on the pupil alpha 1 receptor causes mydriasis and effects aqueous humor productionNorepinephrine


Question Answer
This drug inhibits choline reuptakeHemicholiniums
This drug inhibits the formation Ach vesiclesVesamicol
This drug inhibits the release of Ach from the nerve terminalBotulinum Toxin
Rate limiting step for Ach synthesis isCholine Uptake
Rate limiting step for catecholamine synthesis isTyrosine Hydroxylase
Cholinergic neurotransmission is terminated byAcetylcholinesterase
Adrenergic neurotransmission is terminated byNorepinephrine Reuptake

Cholinergic Drugs

Question Answer
Drugs that act on the receptors itselfDirect Cholinergic Agonist
Drugs that act by inhibiting the metabolism of Ach increases the levels of Ach in synapses and thus increases the actions of AChIndirect Cholinergic Agonists
Acetylcholine, Bethanechol, Pilocarpine (alkaloid), Muscarine (alkaloid), Carbachol, Methacholine are this type of cholinergic agonistsDirect Cholinergic Agonist
Neostigmine, Physostigmine, Pyridostigmine, Edrophonium, Tacrine ,Donepezil Organophosphates - Malathion, Parathion, Sarin are example of drugs that are this type of cholinergic agonistsIndirect Cholinergic Agonist
Methacholine challenge test is use to diagnose this (not actually clinically used)Bronchial Asthma
This drug has strong Muscarinic action & least or no Nicotinic actionBethanechol
This drug can be used to treat Paralytic ileus and Urinary retentions (Non obstructive)Bethanechol
This drug is contraindicated in obstructive urinary retentionBethanechol
Bethanechol is contraindicted in this conditionObstructive Urinary Retention
The mechanism of action for this drug is by stimulating M3 receptors, _________ (this signal pathway) which increasing the bowel movements and bladder contractions facilitates Bethanechol
This drug is an alkaloid and only has Muscarinic activity. It is lipid soluble and penetrates the cornea very wellPilocarpine
This drug can be used to treat glaucoma and Sjogren's syndromePilocarpine
Physostigmine, Neostigmine, Pyridostigmine, Edrophonium, Tacrine, Donepezil and Rivastigmine are these types of cholinesterase inhibitorsReversible Cholinesterase Inhibitors
Malathion, Parathion and Sarin are these types of cholinesterase inhibitorsIrreversible Cholinesterase Inhibitors
Neostigmine, Pyridostigmine and Edrophonium are used to treat this conditionMyasthenia Gravis
This is a short acting Cholinesterase Inhibitors and is used in acute myasthenia gravis cases. Given IVNeostigmine
Used to treat curare toxicityNeostigmine
This is a long acting Cholinesterase Inhibitors. So good for maintenance/ long term therapy. Given orallyPyridostigmine
Used in Glaucoma and atropine overdosePhysostigmine
This drug is a quaternary amine, lipid insoluble therefore not used in glaucomaNeostigmine
This is a very short acting cholinesterase inhibitor. So used in diagnosis of Myasthenia Gravis and to differentiate myasthenic crisis from the cholinergic crisis as part of Tensilon testEdrophonium
This test is done to differentiate myasthenic crisis from Cholinergic crisisEdrophonium
Small doses of edrophonium (1–2 mg intravenously) will produce no relief or even worsen weakness if the patient is receiving excessive cholinesterase inhibitor therapyCholinergic Crisis
Small doses of edrophonium (1–2 mg intravenously) will produce improvement with edrophonium an increase in cholinesterase inhibitor dosage may be indicatedMyasthenic Crisis
Acetyl cholinesterase inhibitors like Tacrine, Rivastigmine and Donepezil are used to treat this conditionAlzheimer's Disease
Of the cholinesterase inhibitor drugs to treat Alzheimer, this drug has hepatic side effectsTacrine
Tertiary amine and lipid soluble. Therefore used in glaucomaPhysostigmine
Decontaminate the skin, do gastric lavage and administer the “Activated charcoal” to prevent unabsorbed drug being absorbed. Give IV Atropine and Pralidoxime is the treatment for thisOrganophosphate Poisioning
This is given to control signs of muscarinic excess stimulation of OP compounds. It should be given IV in large doses until you observe the mydriasis, tachycardia and dryness of mouthAtropine
This drug acts by hydrolyzing (reactivating) the drug bound enzyme. This drug should be given at the earliest possible, that is before “Aging” of the enzyme. If it is given late, has no usePralidoxime
2-PAM-chloride is the also know asPralidoxime
Observation of mydriasis, tachycardia and dryness of mouth seen in a patient indicts thisAtropinization

Anticholinergic Drugs

Question Answer
Atropine, Homatropine, Tropicamide, Pirenzepine, Scopolamine, Benztropine and Ipratropium bromide block this receptorMuscarinic Receptor
A short acting preparation of atropineHomatropine
The shortest acting preparation of atropineTropicamide
Preferred use of this drug in refraction error testing and fundoscopyTropicamide
Used to treat organophosphate poisoning, dilate the eye and for heart block and BradycardiaAtropine
Once used as to treat peptic ulcersPirenzepine
Used to treat motion sickScopolamine
Usually administered 1 hour prior to journey by a transdermal patchScopolamine
Used to treat ParkinsonianBenztropine
DOC of treatment of drug-induced Parkinson's DiseaseBenztropine
Used to treat bronchial asthma and COPDIpratropium Bromide
Used to treat GI spasm, spasmodic abdominal pain Eg: Menstrual painDicyclomaine
The mechanism of action of this drug is competitive blockade of nicotinic receptors (Nn) of ganglionHexamethonium and Mecamylamine
The major side effect of Hexamethonium and Mecamylamine is thisSevere Hypotension
Used as skeletal muscle relaxantsNm Blockers

Adrenergic Drugs

Question Answer
This receptor is found in blood vessels, pupil (Iris) and smooth muscleα1
This receptor is found in presynaptic neuronsα2
This receptor is found in the heart β1
This receptor is found in smooth musclesβ2
This receptor is found in fat tissueβ3
This receptor is found in the renal systemD1
This receptor causes Vasoconstriction produces increased BP, mydriasis, Sphincter contraction which can lead to constipation and Urinary retention. Also is the cause of ejaculationα1
This receptor reduces release of norepinephrine: bradycardia, hypotension. Decreased Insulin release and reduces Aqueous humor productionα2
This receptor increase cardiac conduction as well increases heart rate, force of contraction and cardiac outputβ1
This receptor causes relaxation - bronchodilatation, urinary retention, constipation, uterus relaxation, vasodilation. It also causes gluconeogenesis and glycogenolysis and increases the production of aqueous humorβ2
This receptor causes lipolysisβ3
This receptor causes vasodilation in the renal systemD1


Question Answer
α + β agonistsEpinephrine and Norepinephrine
Selective α1 agonistsPhenylephrine
Selective α2 agonistsClonidine, Apraclonidine, Tizanidine
β agonistsIsoproterenol
Selective β1 agonistsDobutamine
Selective β2 agonistsAlbuterol, Salmeterol,
Dopamine agonistsDopamine


(Insert slide 11-12)
Question Answer
The effects of this drug on the Heart - increases HR, FOC, CO. Blood vessels - Vasoconstriction due to alpha-1 effect Vasodilation predominates in skeletal muscle due to beta-2 effect. BP - In a low dose, decrease in blood pressure. In high dose, increase in mean blood pressure by increasing systolic blood pressure and decreasing diastolic blood pressure. Respiratory system: Bronchial smooth muscle relaxation. GI: Decreased peristalsis (alpha-2 and beta 2) and Contraction of sphincters. Uterus: relaxation in pregnancy (Beta-2): delayed labor. Bladder: Relaxation of detrusor muscle and Contraction of trigone and internal sphincter: urinary retention. Eye: Contraction of radial muscle of iris causing mydriasis (alpha-1). Decreased intraocular pressure due to “reduced” aqueous humor production (alpha-2). In contrast, increased production of aqueous humor due to beta 2 receptor activationEpinephrine
The uses of this drug is for treatment acute hypersensitivity reactions, to retard the absorption of local anesthetics, combine with lidocaine and for cardiac arrestEpinephrine
The effects of this drug direct effects (beta-1) are equal to those of epinephrine. HR,FOC, CO. Indirect effects: In the presence of normal reflex activity, the baroreceptor response to the increased blood pressure overrides the direct effects. “Therefore the final effect is a decrease in heart rate” and no change of a decrease in cardiac output. It has no beta-2 effect.Norepinephrine
The uses of this drug is for treatment for hypotension and vasodilatory shock (due to spinal trauma, spinal anesthesia, sepsis)Norepinephrine
This Alpha-1 Selective Adrenergic Agonist is used for Postural hypotension. As nasal decongestants. As mydriatics in old people and children where atropine is contraindicted. As local vasoconstrictors in case of epistaxisPhenylephrine
This Alpha-2 Selective Adrenergic Agonist is used in Hypertension (2nd choice drug) and withdrawal from tobacco, alcohol or opioids, diazepam. Side effects include postural hypotension, dry mouth, sedation, rebound hypertensionClonidine
DOC in Hypertension in pregnancy. Side effects include postural hypotension, dry mouth, sedation, rebound hypertensionAlpha Methyldopa
A clonidine derivative used in glaucomaApraclonidine
Decreases intraocular pressure due to “reduced” aqueous humor production (alpha-2) and facilitates drainage of aqueous humorApraclonidine
Beta 2 receptor activation increases production of aqueous humor so this beta blocker can be used to treat glaucomaTimolol
Used in Spinal cord spasticityTizanidine
A Non selective beta agonist. Beta-1 mediated increase in heart rate. Beta-2 mediated vasodilation. BP: Reduced DBP, same SBP and reduced mean BP. Can be used in Beta-blocker overdoseIsoproterenol
A selective Beta-1 agonist. Uses is given by IV infusion to patients with cardiac failure or cardiogenic shock who have a severely depressed left ventricular functionDobutamine
A short acting and fast acting Beta-2 Selective Agonists. Used for Bronchial asthma emergency “as needed”. Can also be used in premature labor and in hyperkalemia (shift K+ from extracellular to intracellular space)Albuterol
Beta-2 agonists that can be used to postpone the delivery in premature labor Terbutaline and Albuterol
A slow long acting Beta-2 Selective Agonists. Used for bronchial asthma together with inhaled glucocorticoids in case of moderate or severe asthma. COPD: often used in combination with ipratropium. Can be used in premature labor and hyperkalemia (shift K+ from extracellular to intracellular space)Salmeterol
Side effect of this class of drugs include Tremor ,muscle cramps.Tachycardia, palpitations, flushing, hypotension. Hypokalemia: activation of beta-2 receptors leads to stimulation of K+ uptake into cells, especially skeletal muscle; hypokalemia may have serious consequences in the presence of hypoxia and hypercarbia as in acute asthma. Long-term administration of beta-2 agonists can lead to tolerance development, likely due to “down-regulation” of beta-receptors.Beta-2 Selective Agonists
Activates D1 receptors in low dose. This leads to vasodilation in renal, splanchnic, and coronary beds. In high dose, also activates alpha and beta receptors. Used in shock, when it is associated with poor renal perfusionDopamine
The mechanism of action of this class of drugs - Stimulation of the release of monoamines (norepinephrine, dopamine and serotonin). Blockade of catecholamine reuptake. Uses - Attention deficit / hyperactivity disorders, narcolepsy, weight reductionIndirect-acting Adrenergic Drugs (Amphetamines)
This class of drugs include Amphetamine, Dextroamphetamine (Adderal) and MethylphenidateIndirect-acting Adrenergic Drugs (Amphetamines)
Cheese reaction is due the high concentrations of thisTyramine
An indirect-acting adrenergic drug that block catecholamine reuptake both in the central and peripheral nervous system. Central effects similar to those of amphetamines but shorter lasting and more intense. Inhibits dopamine reuptake into neurons in the "pleasure centers" of the brain. Peripheral actions are similar to norepinephrine. Also has local anesthetic propertyCocaine
An over the counter drug used as nasal decongestant. Tachyphylaxis develops with frequent administration of small dosesEphedrine (Pseudoephedrine)
Ephedrine and Pseudoephedrine belong to this class of drugsMixed-Acting Adrenergic Drugs