autopharm 2 Flashcards

1
Q

what types of adrenergic receptor agonists are there?

A

-alpha agonists: selective and non-selective
-beta agonists: selective and non-selective
-mixed alpha and beta

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2
Q

adrenergic agonists alter what in the cardiovascular system?

A

-rate and force of contraction of the heart; directly and via reflex effects on the heart from actions on vessels
-tone of the blood vessels

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3
Q

what do alpha receptors in most vessels do?

A

facilitate vascular smooth muscle contraction
-increase total peripheral resistance > increase blood pressure > reflex decrease heart rate via vagal reflex

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4
Q

what do beta receptors in blood vessels do?

A

vascular smooth muscle relaxation (skeletal muscle; b2)
-decrease TPR > decrease BP > increase heart rate (direct effect from B1)

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5
Q

equations for BP and CO?

A

BP = CO X TPR
CO = SV X HR

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6
Q

what type of drug is epinephrine? what is it primarily used for?

A

mixed agonist
Activates all a, b subtypes
-Used primarily for cardiovascular support

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7
Q

cardiac effects of epinephrine

A

increase cardiac output by activating β1 force (inotropy) & rate (chronotropy) of contraction

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8
Q

vascular smooth muscle effects of epinephrine

A

Most vessels involve a1 (a2 in some vessels)
> vasoconstriction
> increase TPR

Some vascular beds possess b2 receptors
> vasodilation
> decrease TPR

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9
Q

general smooth muscle effects of epinephrine in the body (aside from vessels); what receptors does it activate and what effects do these have

A

activation of b2 receptors
-bronchodilation
- decrease GI contractions
- decrease tone & contraction of pregnant uterus
- relaxes urinary bladder

activation of a1 receptors:
- contraction of spleen
- contraction of sphincter of the bladder
- contraction of radial muscle of iris (mydriasis)

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10
Q

metabolic effects of epinephrine

A

-increase circulating glucose, lactic acid, free fatty acids

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11
Q

what are important examples of selective beta agonists? what receptors do they work on?

A

Clenbuterol (Ventipulmin®), Terbutaline (Brethine®)
> selective b2

Ractopamine (OptaflexxTM, ActogainTM, Ractopamine 4TM)
>Primarily a b1 agonist with some b2 agonist activity

Dobutamine (generic)
>Relatively selective b1 receptor agonist

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12
Q

what type of drug is clenbuterol? what receptor does it work on and what are its primary uses?

A

Clenbuterol (Ventipulmin®)
-Selective b2 agonists
-Bronchodilators; used primarily for asthma (cats), chronic bronchitis (dogs), lower airway disease (horses)
-Clenbuterol is veterinary approved in horse for oral use as a syrup

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13
Q

what type of drug is terbutaline? what receptor does it work on and what are its primary uses?

A

-Selective b2 agonists
-Bronchodilators; used primarily for asthma (cats), chronic bronchitis (dogs), lower airway disease (horses)
-Terbutaline available as compounded tablets, injectable; small animals

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14
Q

what are the uses for Salbutamol, terbutaline and others used in horses and small animal

A

Inhalant selective b2 agonists available for use as bronchodilators in airway disease

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15
Q

what type of drug is roctopamine? what is its primary use?

A

-Primarily a b1 agonist with some b2 agonist activity
-Increases lean muscle deposition in cattle; growth promotion

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16
Q

what type of drug is dobutamine? what are its uses? what can happen with overdose?

A

Relatively selective b1 receptor agonist
-Used primarily for cardiac support (CHF)
>Improves contractility and BP without significant tachycardia
-Peripheral a1 stimulation possible
-Ventricular tachycardia and hypertension with overdose

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17
Q

what are some important non-selective beta agonists?

A

-Isoproterenol (generic, Isuprel®)

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18
Q

what type of drug is Isoproterenol, and what does it do?

A

generic; isuprel

Non-selective b1, b2 agonist
b1 receptor stimulation
>increase­ inotropy and chronotropy
=>Uses limited to stimulating heart (heart block or bradycardia)
=>But b2 receptor stimulation can yield decreased TPR and overall decreased BP

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19
Q

important selective alpha agonist

A

Phenylephrine (generic, Neo-Synephrine®)

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20
Q

what type of drug is Phenylephrine and what are its effects? how can it be administered?

A

a1 selective agonist

-Oral, injectable, nasal & ophthalmic formulations
-Produces vasoconstriction and ­ BP
> But > reflex decreases heart rate is possible

-May be used for BP support and nasal decongestion
-also pupillary dilation

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21
Q

what kind of drug is dopamine? what does it do?

A

miscellaneous against
-low doses: dilates renal vasculature via D1 receptors > increases­ GFR (glomelular filtration rate)

-moderate doses: b1 receptor effects > increases contractility

-higher doses: a1 agonist > increases TPR (vasoconstriction); increases risk of arrhythmias

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22
Q

what type of drug is ephedrine, psudophedrine, phenylpropanolamine? What do they do?

A

Ephedrine (generic), Pseudoephedrine (generic, Sudafed®), Phenylpropanolamine (Propalin®, Proin®)

-Are classified as direct and indirect acting sympathomimetics
-Can activate a and b receptors as well as promote release of NE from nerve terminals
Available for oral use

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23
Q

generic name for dopamine

A

intropin

24
Q

primary ingredients in ma Huang herb? what is its use?

A

Ephedrine and pseudoephedrine
-herbal preparation available OTC for human and vet products
-Used primarily as nasal decongestants along with anthistamines
-Can be used for urinary tract incontinence in dogs; increases sphincter tone in hypotonic urethra

25
Q

what drug is approved for use in dogs as tablets/syrup for urinary incontinence due to hypotonic urethra in female dogs

A

Phenylpropanolamine

26
Q

what are some therapeutic application of adrenergic agonists?

A
  1. cardiovascular system
  2. respiratory tract applications
  3. anaphylaxis
  4. opthalmology
27
Q

what are the uses of adrenergic agonists for the cardiovascular system?

A

-Treatment of Vascular Hypotension
-Support of Cardiac Insufficiency
-Production of Local Vasoconstriction

28
Q

how can vascular hypotension arise?

A

Hemorrhage
Severe fluid loss
Infection (sepsis)
Adverse drug reactions (see anaphylaxis)

29
Q

how can adrenergic agonists be used to treat vascular hypotension? How does it work? what specific drugs should we use?

A

Treatment of resultant low BP or reduced blood flow
-Expand fluid volume and treat underlying cause is key!
-Can give a1 agonists or vasopressors for short term cardiovascular (cerebral, coronary and renal) support if vasoconstriction is desired…….careful!
-Phenylephrine and Norepinephrine can be used

30
Q

how can adrenergic receptor agonists be used to help with cardiac insufficiency? What specific drugs should we use and for what?

A

b1 receptor agonism may be helpful > increase ­ cardiac contractility & output
-dobutamine or dopamine (acute decompensated CHF)
-isoproterenol (arrest, bradycardia)
-epinephrine (arrest, bradycardia)

31
Q

What can cause cardiac insufficiency?

A

Heart block (bradycardia)
Cardiogenic shock and arrest
Congestive heart failure ?????

32
Q

what class of drugs can produce local vasoconstriction? what specific drugs, and how do they work?

A

adrenergic receptor agonists
-Epinephrine used with local anesthetics (LA)
>Lidocaine HCl 2% with epinephrine > vasoconstriction > decreases blood flow and prolongs LA action at site

  • Epinephrine also used topically to decrease superficial bleeding eg. epistaxis
33
Q

respiratory tract applications for adrenergic receptor agonists

A

i. Treatment of Bronchoconstriction
ii. Nasal Decongestion

34
Q

what class of drugs can be used to treat bronchoconstriction? when are they effective and what is the mechanism?

A

adrenergic receptor agonists
b2 receptor activation > bronchodilation; only effective if bronchoconstriction is present, as occurs with most airway disease

-Clenbuterol (syrup); approved for lower airway disease in horse
-Terbutaline compounded for oral or injectable use primarily for small animal (asthma, chronic bronchitis)
-Salbutamol, salmeterol, terbutaline; inhalants in small animal and horse
-Epinephrine can be given……..risk of tachycardia and arrhythmias; will be used to treat respiratory compromise associated with anaphylaxis

35
Q

what drug treats lower airway disease in horses?

A

Clenbuterol (syrup)

36
Q

what drug is good for asthma, chronic bronchitis in small animals?

A

Terbutaline, compounded for oral or injectable use

37
Q

what can Salbutamol, salmeterol, terbutaline be used for?

A

inhalants in small animal and horse to treat bronchoconstriction

38
Q

what risks come along with using epinephrine for treatment of bronchoconstriction? when is it motly used?

A

risk of tachycardia and arrhythmias; will be used to treat respiratory compromise associated with anaphylaxis

39
Q

what class of drugs is good for treating nasal congestion? what is their mechanism? what specific drugs are used for this purpose? what is a major limitation to their use?

A

adrenergic receptor agonists
a1 receptor activation > vasoconstriction
-Reduce air flow resistance by reducing mucosal edema

Ephedrine, pseudoephedrine and phenylephrine; oral or nasal sprays/drops

Major limitation to their use is “rebound” hyperemia and worsening congestion

40
Q

what class of drugs can be used to treat anaphylaxis (allergic reactions)? What are the general effects?

A

adrenergic receptor agonist

Epinephrine is mainstay of anaphylaxis; usually given IM or IV

-Stabilizes mast cells
-Provides cardiovascular support

41
Q

how are anaphylactic reactions mediated and what are the symptoms?

A

-Are IgE mediated and affect respiratory and cardiovascular systems
-Severe bronchospasm; mucous membrane congestion, angioedema
-Cardiovascular collapse due to vasodilation from mast cell degranulation

42
Q

what drug is used to facilitate retinal examination? how does it work?

A

Phenylephrine (adrenergic receptor agonist)
-a1 activation produces contraction of the radially orientated pupillary dilator muscles of the iris > mydriasis (pupil dilation)

43
Q

what types of adrenergic receptor antagonists are there?

A

alpha antagonists
-non-selective alpha antagonists
selective alpha antagonists

beta antagonists
-non-selective beta antagonists
-selective beta antagonists

mixed adrenergic antagonists

44
Q

what are the general characteristics of non-selective alpha antagonists?

A

-alpha blockade > vasodilation > decreased peripheral resistance and BP
=>reflex tachycardia from reduced BP and blockade of prejunctional a2 receptors

45
Q

what type of drug is Phenoxybenzamine? what is its generic name?

A

Phenoxybenzamine (Dibenzyline®)
-non-selective alpha antagonist

46
Q

what are the properties of Phenoxybenzamine (Dibenzyline®)? what does it do? what are its major uses and adverse effects?

A
  • Irreversible inhibitor of a receptors
  • Has been used for Dx and Rx of pheochromocytoma mediated hypertension
  • Has been used in hypertonic urethra due to functional obstructions or reducing outlet flow resistance with bladder paresis (dog, cat, horse); a1 blockade effect
  • Hypotension is major adverse effect……….careful with “epinephrine reversal”
47
Q

what type of drug is Prazosin? what is its generic name?

A

Prazosin (generic, Minipress®)
-selective alpha antagonist

48
Q

what is Prazosin (generic, Minipress®)? what is it used for? how does it work? what is a possible side effect?

A
  • a1 selective blockade
  • Used for hypertonic urethra due to functional urethral obstruction in small animals
  • May be useful as adjunctive therapy in CHF and pulmonary hypertension
  • Less reflex tachycardia; no effects at prejunctional a2 receptors
  • Hypotension may occur in some patients
49
Q

what type of beta antagonists are important clinically? what are the general characteristics of beta antagonists? what are they used for?

A
  • Drugs with higher affinity for b1 are important clinically
  • Generally well absorbed; low bioavailability from extensive hepatic metabolism
  • Used in cardiovascular disease and ocular conditions
50
Q

what type of drug is Propranolol? what is its generic name?

A

Propranolol (generic, Inderal®)
-non-selective beta antagonist

51
Q

what are the characteristics of Propranolol (generic, Inderal®)? what isits mechanism? what are its clinical uses? what are possible effects?

A
  • Reversible b1 and b2 receptor antagonist; decreased chronotropy and inotropy

Clinical uses in veterinary medicine:
- supraventricular and ventricular tachyarrhythmias
> decrease rate of SA node discharge
> decrease AV conduction and decrease ventricular response to atrial arrhythmias
-decrease sinus node rate; thyrotoxicosis in hyperthyroidism in cats, and pheochromocytoma in dogs
* Hypertrophic cardiomyopathy in cats; relief of outflow tract obstruction
* Bradycardia and hypotension possible; contraindicated in asthmatics, lower airway disease

52
Q

what type of drug its Metoprolol and what is its generic name?

A

Selective b1 antagonist
Metoprolol (generic, Lopressor®)

53
Q

what type of drug is Atenolol and what is its generic name?

A

Selective b1 antagonist
Atenolol (generic, Tenormin®)

54
Q

what are Metoprolol (generic, Lopressor®), Atenolol (generic, Tenormin®) used for? how do they work? what are their effects?

A
  • Relatively selective b1 receptor blockers
  • Produces similar cardiac effects to propranolol
    > Same clinical indications as propranolol
  • Reduced adverse effects such as bronchospasm
    > Bradycardia and hypotension are possible
    > Contraindicated, including propranolol, in significant heart failure unless necessary for tachycardia
  • Atenolol has minimal hepatic first pass effects

Propranolol:
* Reversible b1 and b2 receptor antagonist; decreased chronotropy and inotropy

Clinical uses in veterinary medicine:
- supraventricular and ventricular tachyarrhythmias
> decrease rate of SA node discharge
> decrease AV conduction and decrease ventricular response to atrial arrhythmias
-decrease sinus node rate; thyrotoxicosis in hyperthyroidism in cats, and pheochromocytoma in dogs
* Hypertrophic cardiomyopathy in cats; relief of outflow tract obstruction
* Bradycardia and hypotension possible; contraindicated in asthmatics, lower airway disease

55
Q

what type of drug is Carvedilol? what is its generic name?

A

Mixed adrenergic antagonist
Carvedilol (Coreg®)