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Pharmacology I > Test 2 part IV > Flashcards

Test 2 part IV Flashcards

1
Q

Which category of Alpha Antagonists can be overcome by increasing the concentration of the agonist?

A

Reversible

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2
Q

Most beta antagonists are ______ antagonists, but some are _____ agonists, and there is potential for ______ agonism.

A

Pure (reversible); partial; inverse

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3
Q

Some Beta Antagonists are _____ agonists, meaning they inhibit the action of the receptor in the presence of high catecholamine concentrations, but moderately activate the receptors in the absence of endogenous agonists. It is not yet clear to what extent this is or is not clinically valuable.

A

Partial Agonists

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4
Q

Which Beta Antagonists have the potential to act as inverse agonists?

A
  1. Metoprolol
  2. Betaxolol
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5
Q

Despite some drugs being Beta 1 Specific (MAE), in very high doses, selectivity is _________.

A

Abolished (Selectivity is dose related and diminishes at higher doses)

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6
Q

Most Beta Antagonists resemble which drug at a chemical level to some degree?

A

Isoproterenol

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7
Q

Beta Antagonists are generally ________ absorbed, but do undergo _____ first-pass metabolism

A

Well; Extensive

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8
Q

Beta Antagonists are _______ distributed, with _______ Vd, with half-lives averaging ________.

A

Rapidly; large; 3-10 hours

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9
Q

Which Beta Antagonist is the exception to the usual rule, and is short acting?

A

Esmolol

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10
Q

What metabolizes Esmolol?

A

It is metabolized by hydrolysis in plasma by pseudocholinesterase. Need a decent dose because it immediately is partially metabolized when it’s injected

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11
Q

What are the two types of Cholinomimetic Drugs?

A
  1. Direct Acting
  2. Indirect Acting
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12
Q

What is the mechanism of action for direct acting cholinomimetic drugs?

A

Act directly at either or both the NR or MR. Some drugs are more highly selective for either NR or MR.

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13
Q

Where are Nicotinic receptors located?

A

PNS/SNS Autonomic ganglia, skeletal muscle

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14
Q

Where are Muscarinic receptors located?

A

Sweat glands of SNS, effector organs of PNS

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15
Q

What are the two types of Direct Acting Cholinomimetic Drugs?

A
  1. Choline Esters
  2. Alkaloids
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16
Q

Which type of Direct Acting Cholinomimetic Drugs are either Acetylcholine or structurally similar to Acetylcholine (Exogenous)?

A

Choline Esters

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17
Q

Are the Choline Esters Quaternary or Tertiary?

A

All are Quaternary

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18
Q

What are the example drugs of Choline Esters?

A
  1. Acetylcholine
  2. Bethanechol
  3. Carbocol
  4. Methacholine
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19
Q

Choline esters are all rapidly ______, but each drug will have a varying susceptibility to that, leading to differences in effects on duration of action

A

Hydrolyzed

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20
Q

Which type of Direct Acting Cholinomimetics are Tertiary?

A

Alkaloids

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21
Q

What are the example drugs of the Alkaloids?

A
  1. Nicotine
  2. Muscarine
  3. Lobeline
  4. Pilocarpine
22
Q

What is the mechanism of action of the Indirect Acting Cholinomimetics?

A

Act on Ach-E to prevent degradation of Ach (remember, Ach-E is hanging out in the postsynaptic side of the membrane). End up with increased Ach, PNS is amplified. Some may also have direct stimulating effects on the NR.

23
Q

What are the subtypes of the Indirect Acting Cholinomimetics?

A
  1. Simple Alcohols
  2. Carbamic Acid Esters
  3. Organic Derivatives of Phosphoric Acid
24
Q

What are the reversible types of Indirect Acting Cholinomimetics?

A
  1. Short-acting: Edrophonium
  2. Intermediate-acting: Neostigmine, Pyridostigmine, Physostigmine (Physostigmine is not reversible)
25
Q

Which Indirect Acting Cholinomimetic is Tertiary?

A

Physostigmine

26
Q

Which Indirect Acting Cholinomimetics are Quaternary?

A

All except Physostigmine and Organo-Phosphates

27
Q

Which type of Indirect Acting Cholinomimetics are Irreversible?

A

Organo-phosphates such as Nerve Gases

28
Q

What is the mechanism of action of the Organo-phosphates (Indirect Acting Cholinomimetics)?

A

Forms an irreversible bond with Ach-E, so have to wait for more to be synthesized. Takes a long time.

29
Q

Which drug of the Organo-Phosphate category is non-toxic in ophthalmic form?

A

Ecothiopate is nontoxic in ophthalmic form.

30
Q

Why is Ecothiopate nontoxic?

A

It is highly polar, so not well absorbed. Other organophosphates are toxic.

31
Q

Are the Organo-phosphates well absorbed or poorly absorbed?

A

Well absorbed, can cross the blood-brain barrier. Exception is Ecothiopate which is highly polar.

32
Q

Which Indirect Acting Cholinomimetic is given to treat central anticholinergic toxicity (Central Nervous tissue causing too little Ach)

A

Physostigmine

33
Q

All of the organophosphate (indirect acting cholinomimetics) drugs are well aborbed through the skin, gut, lung, and conjunctiva except for:

A

Ecothiopate

34
Q

Is Neostigmine Quaternary or Tertiary?

A

Quaternary

35
Q

Stimulation of the Muscarinic Receptor causes PNS or SNS effects?

A

Parasympathomimetic effects only

36
Q

Stimulation of the Nicotinic Receptor causes what effects?

A

Autonomic (SNS and PNS) and Somatic Effects

37
Q

What parasympathetic receptor is located more in the brain, and which is located more in the spinal cord?

A

Muscarinic; Nicotinic

38
Q

Which Indirect Acting Cholinomimetic drug forms a covalent bond (long lasting), and has the quality of Aging (AKA, the longer the bond is active, the stronger it gets)

A

Organo-Phosphates

39
Q

What refers to breaking of one of the O2-P4 of the inhibiting agent, further strengthening the covalent bond (Varies by agent)?

A

Aging

40
Q

What kind of bond do Simple Alcohols form?

A

Electrostatic reversible bonds and H+ bonds
Short (2-10 min)

41
Q

What kind of bond to Carbamic Esters form?

A

Covalent bond
Long (30 min - 6 hrs)

42
Q

What are some of the general effects of Ach on Muscarinic Receptors?

A
  1. Inc K+ flux across cardiac cell membranes (Hyperpolarization)
  2. Dec K+ in the ganglion and smooth muscle
  3. Inhibits adenylyl cyclase activity (dec cAMP = no relaxation of smooth muscle, inc GI activity)
  4. Modulates the increase in cAMP by hormones/catechols
43
Q

Muscarinic Receptors use ______, and activate the ________, and cause an increase in _______.

A
  1. G-protein coupling
  2. Activates the IP3 and DAG cascade (Inc Ca+ Release)
  3. Increases cGMP
44
Q

Nicotinic Receptor activation causes:

A

Depolarization of the nerve cell or motor end plate

45
Q

What is the mechanism of action of Nicotinic Receptor Activation?

A

Presence of a NR agonist prevents electrical recovery of the post-junctional membrane = a depolarizing blockade (opens channels and prevents repolarization. Ex: Succinylcholine).
-Refractory to reversal by other agents

46
Q

PNS stimulation of the M3 receptor results in ______, which can be problematic for which patient population?

A

Contraction of the smooth muscle of the bronchial tree and increased tracheobronchial mucosa secretion; Asthmatic Patients

47
Q

Direct Stimulation of the M2 (heart) and M3 (vasodilation) receptors results in what mechanism of action?

A
  1. Increase in K+ to the SA node, AV node, Purkinje cells, atrial and ventricular muscle cells
  2. A decrease in the inward Ca current
  3. A reduction in the hyperpolarization-activated current of diastolic depolarization
    Leads to decreased HR
48
Q

Vasodilation requires _________ to release EDRF (Endothelium relaxing factor)

A

Intact Epithelium

49
Q

What is the mechanism of action of EDRF?

A

EDRF → NO → Guanylyl cyclase → cGMP

50
Q

Why does HTN/Atherosclerosis decrease the release of EDRF?

A

Atherosclerosis damages the endothelium and eliminates the NO/cGMP pathway

51
Q

True/False: Direct slowing of the SA node and AV conduction is opposed by the reflex SNS discharge elicited from the decrease in MAP.

A

True

Pharmacology I (16 decks)

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