Pharmacology-Ch9-Sympathomimetics

Front 1

amphetamine derivatives and tyramine cause the release of this?

Back 1

stored catecholamines

Front 2

what is the mechanism of action of cocaine and TCA's?

Back 2

they inhibit the reuptake of catecholamines by nerve terminals and thus increase the synaptic activity of released transmitter

Front 3

MAO inhibition increases the stores of catecholamines in adrenergic synaptic vesicles what is the effect of this?

Back 3

MAOI's may potentiate the action of indirectly acting sympathomimetics

Front 4

epineprhine has affect at what receptors?

Back 4

all receptor types (a1, a2, B1, B2, B3)

Front 5

what receptors does pheylephrine act at?

Back 5

alpha

Front 6

what receptors does isoproterenol act at?

Back 6

beta

Front 7

dopamine can activate these receptors if given as an intermediate dose?

Back 7

Beta receptors

Front 8

dopamine can activate these receptors if given in large doses?

Back 8

alpha receptors

Front 9

epinephrine, norepinephrine and dopamine are catecholamines that are rapidly metabolized by these enzymes?

Back 9

COMT and MAO

Front 10

do MAOs have an effect on phenylisopropylamines (eg amphetamines)?

Back 10

no amphetamines are resistant to MAO, and most are not catecholamines and so they are also resistant to COMT

Front 11

what metabolizes tyramine?

Back 11

MAO

Front 12

alpha 1 receptor effects are mediated primarily by the trimeric coupling of this protein?

Back 12

Gq

Front 13

what happens when Gq is activated?

Back 13

the alpha moeity of this protein activates phosphoinositide cascade and causes the release of IP3 and DAG from membrane lipids

Front 14

when IP3 and DAG are released what is the effect?

Back 14

calcium is subsequently released from stores in smooth muscle cells and enzymes are activated

Front 15

alpha 2 receptor activation results in this?

Back 15

inhibition of adenylyl cyclase via the coupling of protein Gi

Front 16

Beta receptors (B1, B2, B3) stimulate adenylyl cyclase via the coupling of this protein?

Back 16

Gs

Front 17

what is the effect of Gs activation?

Back 17

Gs activation leads to an increase in cAMP concentration in the cell

Front 18

dopamine D1 receptors activate this in neurons and vascular smooth muscle?

Back 18

adenylyl cyclase in neurons and vascular smooth muscle

Front 19

Dopamine D2 receptors are more important in this location?

Back 19

Brain

Front 20

do catecholamines enter the CNS effectively?

Back 20

no

Front 21

how does the smooth muscle of the pupillary dilator muscle respond to topical pheylephrine and similar alpha agonists?

Back 21

responds as mydriasis (accomodation is not significantly affected)

Front 22

what is the effect of alpha agonists on the flow of aqueous humor?

Back 22

alpha agonists facilitate the outflow of aqueous humor with a subsequent reduciton in intraocular pressure...alpha 2 selective agonists also reduce intraocular pressure apparently by reducing synthesis of aqueous humor

Front 23

how does the smooth muscle of the bronchi respond to B2 agonists?

Back 23

relaxation

Front 24

what is the effect of alpha 2 agonists on the GI tract?

Back 24

they may decrease salt and water secretion into the intestine

Front 25

where are alpha 1 receptors located?

Back 25

most vascular smooth muscle, pupillary dilator muscle, pilomotor smooth muscle

Front 26

where are alpha 2 receptors?

Back 26

adrenergic and cholinergic nerve terminals, platelets, some vascular smooth muscle, fat cells, pancreatic beta cells

Front 27

where are Beta 1 receptors found?

Back 27

heart and JG cells

Front 28

where are Beta 2 receptors found?

Back 28

respiratory, uterine, and vascular smooth muscle, liver, panceratic Beta cells, somatic motor nerve terminals (voluntary muscle)

Front 29

where are Dopamine D1 receptors found?

Back 29

renal and other splanchnic blood vessels

Front 30

where are D2 receptors found?

Back 30

nerve terminals

Front 31

what occurs upon stimulation of D1 receptors?

Back 31

vasodilation (which decreases resistance int eh renal and other splanchnic blood vessels)

Front 32

what is an example of an alpha 1 agonist?

Back 32

phenylephrine

Front 33

what is the effect of phenylephrine?

Back 33

constriction of skin and splanchnic blood vessels and increase peripheral vascular resistance and venous pressure. - they often invoke compensatory reflex bradycardia

Front 34

what is an example of an alpha 2 agonist?

Back 34

clonidine

Front 35

what is the action of clonidine?

Back 35

cause vasoconstriction when administered IV or topically (as a nasal spray), but when given orally they accumulate in the CNS and REDUCE sympathetic outflow and blood pressure

Front 36

give an example of a Beta 2 agonist?

Back 36

terbutaline

Front 37

what would be the effect of norepinephrine (both alpha and beta1 effects) on the heart?

Back 37

may cause reflex increase in VAGAL outflow because they increase blood pressure and evoke the baroreceptor reflex

Front 38

a pure alpha agonist (phenylephrine) will often have this effect on heart rate?

Back 38

slows through the baroreceptor reflex

Front 39

pure beta agonists (eg isoproterenol) almost always has this effect on heart rate?

Back 39

it increases heart rate

Front 40

what effect do B1 agonists have on renin secretion?

Back 40

B1 agonists increase renin secretion

Front 41

what effect do Beta2 agonists have on the pancrease?

Back 41

they increase insulin secretion by the pancreas

Front 42

what is the drug of choice in anaphylactic shock?

Back 42

epinephrine

Front 43

epinephrine and this prodrug have been used topically in the treatment of glaucoma?

Back 43

dipivefrin

Front 44

what are the newer alpha2 agonists introduced for use in glaucoma?

Back 44

apraclonidine and brimonidine

Front 45

what is the recommended prophylaxis for asthma?

Back 45

a longer acting B2 selective agonist called Salmeterol (not recommended for acute symptoms)

Front 46

what are the B2 selective agonists that are NOT recommended for prophylaxis but are sage and effective and lifesaving in the treatment of bronchospasm?

Back 46

short acting B2 agonists = terbutaline, albuterol, and metaproterenol

Front 47

what type of sympathomimetic would you use in the case of ACUTE heart failure and some types of shock?

Back 47

Beta 1 agonists = they increase cardiac contractility and reduce (to some degree) afterload by decreasing the impedance to ventricular ejection through a small B2 effect)

Front 48

this type of sympathomimetic is used with local anesthesia to reduce the loss of anesthetic from the area of injection?

Back 48

alpha agonists

Front 49

chronic orthostatic hypOtension due to inadequate sympathetic tone can be treated with these two things?

Back 49

ephedrine or a newer orally active Alpha 1 agonist, midodrine

Front 50

what are some examples of Beta 2 agonists that are used to suppress premature labor?

Back 50

ritodrine and terbutaline

Front 51

give some other examples of non sympathomimetic agents that can be given to suppress premature labor?

Back 51

NSAIDS, calcium channel blockers, and magnesium

Front 52

long acting oral sympathomimetics such as ____ are sometiems used to improve urinary continence in children with enuresis and in the elderly

Back 52

Ephedrine

Front 53

what mediates the anti eneurisis action of ephedrine?

Back 53

alpha receptors in the trigone of the bladder and in men the smooth muscle of the prostate

Front 54

alpha 1 agonists can have this side effect?

Back 54

hypertension

Front 55

beta 1 agonists can have this side effect?

Back 55

tachycardia and serious arrhythmias

Front 56

B2 agonists can have this side effect?

Back 56

skeletal muscle tremor

Front 57

what are the major toxicities of cocaine?

Back 57

cardiac arrhythmias or infarction and convulsions.

Front 58

what two drugs are used for shock and heart failure?

Back 58

Dopamine and Dobutamine

Front 59

what drug is used for narcolepsy, obesity and ADD?

Back 59

Amphetamine, phenmetrazine and others

Front 60

what drug is used to cause mydriasis, vasoconstriction and decongestions?

Back 60

Phenylephrine

Front 61

what drugs are used for asthma?

Back 61

albuterol, metaproterenol, and terbutaline

Front 62

what drugs are used to cause nasal decongestion (long action)?

Back 62

oxymetazoline, and xylometazoline

Front 63

what drug is used to cause vasoconstriction and is used as a local anesthetic?

Back 63

cocaine

Front 64

what drug is used to cause vasoconstriction in hypOtension?

Back 64

norephinephrine

Front 65

what drug is used for asthma and AV block?

Back 65

isproterenol

Front 66

what drug is used for anaphylaxis, glaucoma, astham and to cause vasoconstriction?

Back 66

catecholamines, epinephrine

Front 67

what drug is used for urinary incontinence and to cause vasoconstriction in hypOtension?

Back 67

ephedrine

Front 68

which drug is a direct Alpha1, a2, B1 and B2 agonist?

Back 68

epinephrine

Front 69

what drugs are an indirect catecholamine releasers?

Back 69

**Tyramine, also amphetamine and ephedrine

Front 70

what drugs are indirect catecholamine uptake inhibitors?

Back 70

**Cocaine, also TCAs

Front 71

which drug has more alpha 1 action than alpha 2?

Back 71

phenylephrine (also mehtoxamine, metaraminol and midodrine)

Front 72

which drug has greater alpha2 than alpha 1 action?

Back 72

clonidine

Front 73

which drug has equal B1 and B2 action?

Back 73

isproterenol (B1 = B2 actions)

Front 74

which drug has greater B1 than B2 action?

Back 74

dobutamine

Front 75

which drug has greater B2 than B1 action?

Back 75

terbutaline (also albuterol, metaproterenol and ritodrine)

Front 76

which drug is a dopamine agonist?

Back 76

dopamine and bromocriptine