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Pharmacy School 2015-16 > PHAR 736 Exam 1 > Flashcards

PHAR 736 Exam 1 Flashcards

1
Q

a1 tissue locations and corresponding effects

A

Major blood vessels and vasculature in dermal, GI, renal, bladder and nasal membranes (constriction, increase peripheral resistance, increase diastolic BP)

Eye (contraction of radial muscles –> mydriasis)

Bladder and GI sphincters (constrict sphincters, decrease outflow)

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2
Q

a2 tissue locations and corresponding effects

A

Eye (decrease aqueous humor production)

Pancreatic islets (decrease insulin release, increase blood glucose)

Presynaptic nerve terminals (decrease NT release, e.g. NE)

CNS/brainstem (decrease blood pressure/inhibit baroreflex)

Spinal cord (inhibit pain transmission)

Nasal vasculature (constriction)

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3
Q

B1 tissue locations and corresponding effects

A

Heart (increase HR, increase contractility, increase force –> increase CO)

Kidney (increase renin secretion –> vasoconstriction)

Eye (increase production of aqueous humor)

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4
Q

B2 tissue locations and corresponding effects

A

Hepatic and skeletal muscle - vascular smooth muscle (relaxation, increased blood flow to liver and skeletal muscle)

Pulmonary smooth muscle (relaxation –> increased airflow)

GI long smooth muscle (relaxation, decreased motility)

Bladder detrusor muscle (relaxation, decreased outflow)

Pregnant uterus (relaxation)

Skeletal muscles (increased glycogenolysis, increased K+ intake)

Mast cells (decreased degranulation)

Pancreas (increased glucagon secretion)

Liver (glycogenolysis –> increase in blood glucose)

Eye (increase production of aqueous humor)

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5
Q

Somatic Nervous System

A

Innervation of striated (skeletal) muscle

Control of voluntary movement

No ganglia between spinal cord and target

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6
Q

Autonomic Nervous System

A

Innervation of smooth muscle, glands, organs, blood vessels, fat and skin

Involuntary bodily functions (respiration, BP, secretions, body temp, digestion, heart rate)

Sympathetic division (SNS) produces fight or flight response | adrenal medulla functions like sympathetic ganglion but releases epinephrine into bloodstream

Parasympathetic (PNS) produces rest and digest state | target organs are activated as needed

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7
Q

Describe parasympathetic innervation/cell bodies

A

Long pre-ganglionic neuron

ACh released at ganglion and at target organ | Neuronal nicotinic receptor on post-ganglionic neuron | Muscarinic receptor at target organ

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8
Q

Describe Sympathetic Innervation/cell bodies

A

ACh released at ganglion | NE released onto alpha and beta receptors OR EPI released by adrenal medualla into blood | short pre-ganglionic neurons

Neuronal nicotinic receptors on ganglia and adrenal medualla

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9
Q

Describe somatic innervation/cell bodies

A

1 long neurone | releases ACh onto muscular nicotinic receptor located on striated muscle

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10
Q

ACh is used by all neurons that originate in the ______________

A

Spinal cord

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11
Q

Ganglia in the PNS

A

Ganglia are close to target organs due to long pre-ganglionic neurons, therefore, target organs are discretely activated

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12
Q

Define ganglia

A

Collections of synapses protected by a barrier

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13
Q

Basal tone at rest of most organs is __________________

A

parasympathetic

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14
Q

In GI and bladder sphincters, the _____ indirectly controls the _____

A

PNS

SNS

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15
Q

The SNS __________ insulin and _________ glucagon

A

inhibits; stimulates

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16
Q

Decrease in secretions of eye is SNS or PNS?

A

SNS

Decreased secretions = better visual acuity

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17
Q

PNS and SNS cooperation

A

Sweat: generalized skin hydration by PNS, localized sympathetic cholinergic sweating in palms and underarms

Pulmonary secretion: PNS control mucus secretions in lungs, SNS controls watery secretions

Male Sex Response: Point and Shoot

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18
Q

Pregnany uterine myometrium inhibited with ____ stimulation

A

SNS

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19
Q

Exclusive __________ control of major blood vessels

A

sympathetic; they provide basal tone

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20
Q

Sympathetic innervation of skeletal muscle and liver is _____________

A

vasodilating

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21
Q

Skeletal muscle metabolism controlled by _________________ nervous system

A

sympathetic

22
Q

Partial agonists tend to cause very little receptor

A

Desentiziation

23
Q

Supersensitization occurs with ___________

A

antagonists

beta-blockers are most relevant (increases likelihood of MI for 2 weeks following)

24
Q

Agonists tend to cause _______________

A

desensitization

25
Q

How does the body prepare for blood loss? (which adrenergic receptors)

A

a2 mediated potentiation of platelet aggregation

b1 mediated increases in renin secretion leading to vasoconstriction

26
Q

Norepinephrine

A

a1 a2 and b1 activity

Useful in hypotensive crisis, as seen in SNS degenerative disease

Only vasoconstrictive effects

27
Q

Epinephrine

A

Activity at all adrenergics

First-line in anaphylactic shock and acute cardiac arrest

Supports BP and maintains cardiac perfusion

28
Q

Droxidopa

A

Approved for neurogenic orthostatic hypotension, including autonomic degeneration

Converted to NE and EPI in CNS and PNS

Only proven useful for 2 weeks

29
Q

Isoproteronol

A

Beta selectivity

Useful in severe bradycardia, especially heart block, to raise HR and CO

Does NOT support blood pressure; reduces BP

30
Q

Dopamine

A

Drug of choice for hemodynamic shock and useful for septic shock

Administer with plenty of fluid

Low dose = D1 agonist (increase renal blood flow and perfusion, increase coronary blood flow)

High dose = b1 agonist

Highest dose = a1 agonist (increase vasoconstriction to support BP, may have detrimental effects on renal perfusion)

31
Q

Dobutamine

A

Used for systolic dysfunction in those with late-stage CHF (for patients who cannot tolerate an increase in heart rate; has similar b1 agonism effect to NE)

Only use for 4 days

S (-) isomer = B1/B2/a1 agonism
R(+) isomer = B1/B2 agonism; a1 antagonism

R = 10x more potent than S

32
Q

b2 Sympathomimetics contraindications

A

Coronary artery disease (some b1 activation will occur)

Patients currently on b-blocker, MAO inhibitor, or tricyclic antidepressant

Hyperthyrdoisim

Diabetes (b2 will increase blood sugar through increased glucagon secretion)

Glaucoma (b2 will increase aqueous humor production)

33
Q

b2 sympathomimetic side effects

A

CNS stimulation (includes headache)

Tachycardia and arrhythmias

Electrolyte imbalances (hypokalemia)

Nervous muscle twitches due to hypermatbolic state of skeletal muscles

Decreased bronchoplasticity from chronic use may exacerbate symptoms in long run

34
Q

Terbutaline

A

Tocolytic agent; b2 agonist

Used off label to prevent labor for up to 48 hours

No use beyond 48 hours due to receptor desensitization

Also used in status asthmaticus (patient is unable to move air and may be unconscious)

35
Q

SABAs

A

Desensitization if used to often, may lead to non-compliant airways

Albuterol, Ventolin and Metoproterenol

Inhalers

Terbutaline also used if patient can’t move air (subcu or IV)

36
Q

LABAs

A

Good for night time therapy

Longer time of onset

Formoterol, Formoterol + Budenoside steroid

Receptor desensitization controlled by concurrent administration of steroids

Salmeterol is partial agonist with little desensitization; slower onset (20 minutes) compared with formoterol (6-7 minutes)

37
Q

Ultra long acting b2 agonists for COPD

A

Indacaterol, VIlanterol (partial agonists with little receptor desensitization)

Once daily dosing

Faster onset of activity similar to formoterol (~6-7 minutes)

38
Q

No true ____ selective agonists with therapeutic utility

A

B1

39
Q

B2 selective sympathomimetic indications

A

Asthma and COPD
Acute respiratory distress
Allergic reactiosn
Uterine hyperactivity in premature labor

40
Q

a1-selective sympathomimetic indications

A

Nasal congestion
Hypotension
Tachycardic arrhythmias, specifically PAT (increased BP = reflex bradycardia)
Adjuvants with topical anesthetics (vasoconstriction maintains local concentration of topical anesthetics)
Mydriatic for eye exams

41
Q

a-1 selective sympathomimetic contraindications

A

Hypertension

42
Q

a1-selective sympathomimetic side effects

A

Appetite suppression (reduced GI bloodflow)

Urinary retention (constriction of bladder sphincter)

Bradycardia and arrhythmias

Photophobia (from mydriasis)

CNS effects (nervousness, tremors, irritability, sweating)

Rebound congestion after discontinuation

43
Q

Midodrine

A

Approved for orthostatic hypotension

44
Q

Phenylephrine

A

Cyclomydril when used for eye exams

Direct a1 agonist nasal and ocular decongestant

Poor oral bioavailability

45
Q

Tetrahydrazoline, Oxymetazoline

A

Ocular decongestants

Nasal decongestants (a1 and a2 activity)

Rebound congestion may be problem; possible tissue necrosis with chronic use

Loss of smell reported in some cases

46
Q

a2-selective agents (general)

A

Considered sympatholytic agents

Lower BP by inhibiting NE release through a2 autoreceptors; block baroreflex so little effect on HR; CNS effects lead to lower BP; CNS effects calming, sedating and reduce anxiety; spinal cord effects decrease muscle spasms and reduce hyperalgesia

47
Q

a2-selective agonist indications

A

Hypertension (CNS and autoreceptor effects) –>even more effective under stress by decreasing NE release onto heart

Glaucoma

Drug and alcohol withdrawal (reduce anxiety, hyperalgesia, and tachycardia)

ADHD (patients may benefit from calming)

Anti-spastic agents (decrease hyperalgesia associated with muscle spasm)

Dermal flushing (useful in perimenopausal women)

48
Q

a2-selective agonist contraindications

A

Diabetes (decrease insulin release from pancreas)

49
Q

a2-selective agonist side effects

A

Postural hypotension and suppressed heart rate (blocks bodies ability to compensate for gravitational effects from sitting or standing; huge problem in elderly with stiff arteries and compromised baroreflex)

Rebound hypertension

Sedation (sympatholytic CNS effects)

50
Q

Contributors to long duration of LABAs (b2 agonists)

A

1) No COMT
2) No MAO
3) High lipophilicity from extended substituent on nitrogen = prolonged and selective binding to second non-polar domain on b2 receptor
4) Greater bronchiol tissue penetration leading to decreased clearance from lungs

Pharmacy School 2015-16 (34 decks)

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