Sympathomimetic Agents

Front 1

Epinephrine- Class, MOA(receptors), PK

Back 1

Class: direct acting sympathomimemtic-- adrenergic receptor agonist
MOA: acts equally at all receptors--alpha1, beta1, alpha2, beta2
PK: at low infusions will reach EXTRAsynaptic receptors--alpha2 and beta 2 preferentially over alpha 1 and beta 1

Front 2

NE- Class, MOA (receptors), PK

Back 2

Class: Direct acting sympathomimetic
MOA: works at all receptors except not at beta 2
PK: have similar effects at heart at low and high rates of infusion

Front 3

Isoproterenol- Class, MOA (receptors), PK

Back 3

- Class: Direct acting sympathomimetic
MOA: stimulates all beta but not alpha receptors
PK: similar effects at heart at low and high rates of infusions

Front 4

Dopamine- Class, MOA (receptors), PK

Back 4

Class: Direct acting sympathomimetic
MOA: Dopamine receptors>Beta 1> alpha 1>>all others)
PK: at low doses will stimulate D receptors in GI AND RENAL ARTERIES than beta 1 (which may also stimulate contractility in the heart) then alpha 1 (vascular effects)

Front 5

Dobutamine- Class, MOA (receptors), PK

Back 5

Class: Direct acting sympathamimetic
MOA: selective beta 1 agonist-- B1 much more than beta 2
PK: administered as stereoisomer mix so that it is pretty specifically stimulates beta-- so that cardiac contractility is increased WITHOUT increase in diastolic pressure (i.e. in TPR) b/c alpha receptors are not activated

Front 6

Epi- Class, Use

Back 6

Class: nonselective sympathomimetic
Use: main is that Epi causes bronchodilation via beta 2. Anaphylactic shock (at high dose), bronchoconstriction in asthma, cardiac arrest, at high dose to treat badycardia due to AV block until pacemaker can inserted, and also is mixed with local anesthetics to prolon action at local site of injection b/c the epi will cause vasoconstriction and keep the anaesthetic in teh local area

Front 7

NE: Class, Use

Back 7

Class: non selective sympathomimetic (all receptors except beta2)
Use: most though not all uses due to effects on vascular system via alpha 1, used for shock--using cardiac beta1 and vascular alpha receptors, support of BP during spinal anesthesia

Front 8

Isoproterenol- Class, Use

Back 8

Class: direct sympathomimetic- is more selective for beta 1 and beta 2, Use: main is pharmacological provocation to assist with unexplained syncope

Front 9

Dopamine- Class, Use

Back 9

Class: D receptors, Beta 1, then alpha 1--then all others-- direct sympathomimemtic
Use: certain types of shock, CHF (if refractory to other forms of therapy), bradycardia treatment if unresponsive to other treatment

Front 10

Dobutamine- Class, Use

Back 10

Class: direct sympathomimetic selective beta 1 agonist
Use: Like dopamine, used in CHF and certain forms of shock (for example, cardiogenic and late phase septic) though only targeting cardiac β1. Sometimes used to stimulate the heart during emergence from surgery.

Front 11

Albuterol- Class, MOA (receptors), PK

Back 11

Class: direct acting sympathomimetic
MOA: selective beta 2 agonist- then some beta 1
PK: Oral, IV, and inhaled

Front 12

Phenylephrine- Class, MOA (receptors),Pk

Back 12

Class: Direct acting sympathomimetic
MOA: selective alpha 1 agonist--vascular effects most intense
PK: IV, oral, topical, spray (poor oral absorption though)

Front 13

Cocaine: Class, MOA, PK

Back 13

Class: Indirect acting sympathomimetic
MOA: inhibits reuptake of NE at sympathetic nerve terminals
PK: local anesthetic agent (listed as a topical anesthetic for mucous membranes), it can potentially (through above inhibitory action on reuptake of peripheral NE) exert its own local vasoconstrictor action at site of local injection, retarding its own loss from site.

Front 14

Pseudoephedrine and ephedrine: Class, MOA, Use

Back 14

Class: Indirect acting sympathomimetic
MOA:like tyramine, stimulate release of NE from sympathetic nerve endings independent of nerve action potentials but also stimulate adrenergic receptors directly.
Use: treat nasal and bronchial congestions. Promotes nasal and sinus drainage.

Front 15

general PK considerations for sympathomimetics

Back 15

1. In general, the selective α1 and Beta 2 direct-acting agonists and indirect-acting drugs (except cocaine) may be readily absorbed after swallowed oral administration and may last for hours in terms of duration of therapeutic action. Salmeterol very long duration.
2. To be effective therapeutically, cocaine plus the other direct-acting agonists (e.g. E, NE, Isoproterenol, DA, Dobutamine) must usually be given parenterally. Typically, their actions last only a few minutes if given intravenously (due to rapid inactivating mechanisms) though usually longer if injected directly into whole tissue (e.g. E into skeletal muscle or mucosa).

Front 16

Albuterol- Use, Receptor, Class

Back 16

Use: Bronchodilation for asthma and COPD via BETA 2 receptors
Class: selective beta 2 agonist

Front 17

Terbutaline- Use, receptor, Class

Back 17

Use: Bronchodilation for COPD and asthma and uterine RELAXATION (used to stop premature labor) via BETA 2 receptors
CLass: Selective beta 2 agonist

Front 18

Phenylephrine and midodrine- Use, receptor, class

Back 18

Use: to raise diastolic with reflexive bradycardia,
- used to treat supraventricular tachycardia-- really high heart rate due to SA node, so with this will have reflexive decrease in heart rate
- used during neurogenic shock or during spinal anesthesia
- treat nasal congestion by VASOCONSTRICTING nasal vessels
- also dilates pupiles by constricting the dilator pupil muscle
- also midodrine to treat orthostatic hypotension
CLASS: SELECTIVE alpha 1 agonist

Front 19

Cocaine- Use, MOA

Back 19

Use: local anaesthetic
MOA: Cocaine acts as an aesthetic.Furthermore, it will inhibit hte re-uptake of NE allowing the NE to exerts its vasoconstrictor effects -- this allows cocaine to act both as a local anesthetic and its own vasoconstrictor

Front 20

Pseudoephedrine- Use, MOA, Side effect

Back 20

MOA: stimulate release of NE from nerve terminals without APs by reversing the reuptake at nerve terminals-- leads to vasoconstriction of nasal mucosa-> decongestion
Side effects: raise BP, and heart rate

Front 21

SElective alpha 1 and beta 2 agonists and indirect agonists (pseudoephedrine) have what PK

Back 21

oral is fine and last for a few hours

Front 22

Selective beta 1, cocaine, and non selective agonists have what PK

Back 22

PK: must be give parenterally and act only for few minutes

Front 23

Timolol- Use, Class

Back 23

Class: Beta blocker
Use: To decrease intraocular pressure, used b/c it does not have membrane stabilization effects (anesthetic in eye would be bad)

Front 24

Phenoxybenzamine, Phentolamine (Oraverse)- Use, Class

Back 24

Class: NON SELEctive alpha 1 and alpha 2 blockers
Use: can treat tissue dermal necrosis associated with injecting NE into tissue which would cause crazy vasoconstriction and necrosis
- used also to combat pheochromacytoma when too much E being produced and severe HTN
- oraverse- reverse dental anesthesia by stopping vasoconstriction and allowing dissipation of local anesthetic

Front 25

Prazosin- Class, Use, Side effects

Back 25

Class: -OSIN drig-- selective alpha 1 blocker
Use: to help relax urinary sphincter muscle in BPH
Side effects: Orthostatic hypotension, generalized edema, reflexive tachycardia, problems with ejaculation (shoot)

Front 26

TAMsulosin and silodosin- Class, Use, Side Effects

Back 26

- CLass: ALPHA 1 Subtype A BLOCKER
USE: flomax-- helps to pee in BPH
SIde effects: less than with prazosin (no orthostat hypotension) but will see vas deferens probs still-- ejaculation problems

Front 27

Alfuzosin- CLass, USe, side effects

Back 27

Class: Alpha 1 A blocker
USE: increase urine flow in BPH, accums in prostate
Side effects: do not have ejaculatory problems as with tamsulosin and silodosin BECAUSE alfuzosin only accums by prostate not in vas deferens