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Session 2 Pharm8
Pharm -8- Adrenergic Agents
| Question | Answer |
|---|---|
| What is an indirect-acting adrenergic agent | drug enhances the release of norepi from vesicles |
| What is a mixed acting adrenergic agent | Drug acts both indirectly causing increased release of nor epi and directly activating receptors |
| What is a direct acting adrenergic agent | drug activates adrenergic receptors |
| What are the two classes of adrenergic agonists | selective and non-selective |
| What are the four type of adrenergic receptors that selective adrenergics can be target at | alpha 1, A2, B1 and B2 |
| Main effect of activating this adrenergic receptor type is, -vasoconstriction -mydriasis -relaxation of GI smooth muscle (except sphincters -Thick viscid salivary secretions -hepatic glycogenolysis -decrease renin release -ejaculation | Alpha ! receptor activation |
| The main effects of activation of this adrenergic receptor is, -inhibition of transmitter release, -vasoconstriction -platelet aggregation -inhibition of insulin release -ejaculation | Alpha 2 receptor activation |
| The main effects of activating this adrenergic receptor is -incresed cardiac rate and force -increased renin release | Beta 1 receptor activation |
| The main effects of activating this adrenergic receptor is -bronchodilation -vasodilation -relaxation of visceral smooth muscle -hepatic glycogenolysis -skeletal muscle tremor | Beta 2 receptor activation |
| The main effect of activating this adrenergic receptor is -lipolysis | Beta 3 receptor activation |
| What are the non selective adrenergic agonists | Epinephrine, Nor epi, Isoproterenol, Oxymetazoline |
| What receptors will Epi activate | alpha 1, 2 and B1 and B2 |
| What recetpors will nor epi activate | A1, A2 and B1 |
| What receptors will isoproterenol activate | B1 and B2 |
| What Receptors will oxymetazoline activate | A1, and A2 |
| what are the clinical uses for epinephrine | Reserved for emergency situations -cardiac resuscitation -treat hypersensitivity reactions (anaphylaxis) -relieve bronchospasm in acute asthma -reduce IOP in glaucoma -prolong duration of anesthesia -topical hemostatic agent |
| What is the MOA of epinephrine | based on actions on blood vessels, heart and bronchial smooth muscles |
| What are the pharmacokinetics of Epi | rapid onset of action short duration of action-rapid inactivation by liver MAO- COMTs Cannot be given orally- gets inactivated my MAOs and COMT in the gut |
| What are the s/e of EPI | hypertension, reflex bradycardia, tachycardia, ventricular arrhythmia's, tremor, hyperglycemia |
| What are the clinical uses of Norepi (levophed) | Reverses hypotension in shock but limited therapeutic value |
| What are the clinical uses of isoproterenol | used for asthma but albuterol is better used for cardiac resuscitation |
| What is oxymetaqzoline | non selective A1 and A2 agonist common ingredient in nasal decongestants |
| What is the MOA of oxymetazoline | constricts the small arterioles supplying the nasal mucosa, decreasing secretions. |
| What are the limiation of using oxmetazoline | Loss of eficacy with chronic use (desensitization of alpha receptors) Rebound hyperemia and worsening of symptoms |
| What are PHENYLEPHRINE methoxamine metaraminol midodrine | selective Alpha 1 agonists |
| What are CLONIDINE APRACLONIDINE brimonidine guanfacine guanabez methyldopa tizanide | selective A2 agonists |
| What are the clinical uses of PHENYLEPRINE | nasal decongestant, mydriatic agent, can be used in short term hypotensive emergencies, or to maintain B/P in spinal anesthesia |
| What is the advantage of using phenylephrine as a nasal decongestant over oxymetaxzoline | Phenylephrine does less mucosal damage |
| How does phenylephrine compare to atropine as a mydriatic agent and when is it contraindicated | it cause pupil dilation (mydriasis) without loss of accomodation. Contraindicated in narrow angle glaucoma |
| What is the MOA of phenylephrine | based on its ability to selectively activate A1 receptors causing vasoconstriction of nasal mucosa and contraction of radial muscle |
| What is the Clinical use of CLONIDINE | treat hypertension, and treating addicted patients for withdrawl from narcotics, alcohol and tobacco |
| what is the MOA of Clonidine | partial agonist of A2 receptors, acts at presynaptic alpha 2 receptor to reduce NE release at vasculature, But main effect is at A2 receptors in brainstem nuclei to decrease sympathetic outflow to heart and vasculature |
| can Clonidine cross the BBB | yes |
| Is clonidine absorbed orally | yes reaches a peak in about 2 hours |
| what administration of clonidine is used to reduce CNS side effects | transdermal patch |
| What are the s/e of clonidine use | dry mouth, sedation, marked bradycardia, sexual dysfunction |
| why can't you suddenly stop clonidine treatment | abrupt dc after long term therapy can cause rebound hypertension |
| What type of adrenergic agonist is apraclonidine(iopidine) and what is it clinically used for | selective A2 agonist, topically sued to reduce IOP in patients with open angle glaucoma |
| What is the MOA of apraclonidine(iopidine) | reduce aqueous humor production by acting @ post synaptic A2 receptors to cause vasoconstriction in the ciliary epithelium. Does not cross BBB and has fewer CNS s/e |
| What are dopamine and dobutamine | selective B1 agonists |
| What are terbutaline, alubeterol, pirbuterol, bitolterol, fenoterol, formoterol, Salmeterol, and ritodrine | B2 selective agonists |
| catecholamine the is the metabolic precursor to Nor epi and Epi also synthesized in epithelial cells of the proximal tubule causing local diuretic and natriuretic effects | Dopamine |
| What are the effects of dopamine on the vsculature, Renal, and B1 adrenergic receptors | vasculature-(renal, mesenteric, coronayr) D1 recepetor causing vasodilation Renal D1 receptor- on thick ascending limb and loop of henle inhibit Na pump and Na/H exchanger B1 adrenergic receptor- positive ionotropy increases contractility |
| What are the clinical uses of dopamine | improve cardiac and renal function in critical patients with CHF and Renal failure Used to help treat cardiogenic and septic shock after fluid replacement therapy |
| Drug that resembles dopamine but is a mixture of several enantiomers and is more selective for B1 receptors | Dobutamine |
| What are the enantiomers of dobutamine selective for | "-" enantiomer is potent A1 agonist "+" enantiomer is potent A1 antagonist both are agonists at B1 receptor |
| How does Dobutamine compare to isoproterenol in CVS effects | more prominent ionotropic (contractility) effects than chronotropic (rate) effects on heart peripheral resistance in not greatly affected |
| what are the clinical uses of dobutamine | short-term management of cardiac decompensation that may occure after cardiac surgery -CHF -Myocardial infarction |
| What does dobutamine essentially do | increases CO and SV without increasing HR or BP |
| What are the clinical uses of Albuterol (Ventolin) and what type of drug is it | Albuterol a B2 selective agonist is used to relieve bronchospams associated with asthma and COPD by stimulating bronchodilation |
| What is the clincal use of Salmeterol(serevent) and what type of drug is it | Selective B2 agonist in is used to relieve bronchospasm in asthma and improve lung function in COPD. |
| What is the MOA of salmeterol (serevent) | acts on B2 receptors and has anti-inflammatory properties longer duration of action than albuterol but slow onset of action |
| Selective B2 agonist developed to specifically cause uterine relaxation and help arrest premature labor | Ritodrine |
| What are the S/E of B2 agonists | increased heart heart (via B1 stimulation) Tremor (B2) Decreased plasma [k] (B2) increase plasma [glucose] (B2) |
| What are phenoxybenzamine and phentolamine | non selective A1 an A2 antagonists |
| What are- PRAZOSIN (Minipress) Terazosin (Hytrin) Doxazosin (Cardura) Alfuzosin TAMSULOSIN (Flomax) Indoramin Urapidil Bunazosin | selective A1 antagonists |
| what is Yohimbine | Selective A2 antagonist |
| What is the clinical use of Phenoxybenzamine | treat pheochromocytoma |
| What is the MOA of phenoxybenzamine | as a non-selective Alpha receptor antagonist it is an irreversible antagonist at alpha receptors decreases preload |
| What are the S/E of phenoxybenzamine | postural or orthostatic hypotension reflex tachycardia Tachycardia Vertigo Sexual Dysfunction |
| What are the clinical uses of the selective A1 antagonist Prazosin | used to treat essential hypertension, CHF, and BPH |
| What is the MOA of prazosin | Blocks A1 receptor (selective A1 antagonist) in arteries and veins and decreases preload, evokes less reflex tachycardia then phenoxybenzamine (no A2 antagonism) -Also acts in CNS to suppress sympathetic outflow -Favorable effects on lipid profile |
| What are the S/E of Prazosin | First dose phenomena- marked postural hypotension, and syncope in 30-90 min after first dose -limit initial dose, gradually increase the dose to achieve antihypertensive goal, |
| What are the clinicla uses of Tamsulosin (flomax) a selective A1 antagonist | used for symptomatic relief of urethral obstruction in Benign Prostatic Hyperplasia BPH |
| What is the MOA of tamsulosin (flomax) | blocks A1 receptors on the trigon, internal sphincter and prostate smooth muscle |
| What is benign Prostatic hyperplasia | increased smooth muscle mass of the prostate puts pressure on urethra, increase A1 mediated tone of the prostate, and Activation of A1 receptors on trigone and sphincter leading to -weak stream of urine -frequent urination -nocturia |
| What are PROPRANALOL TIMOLOL Pindolol Nadalol | Non-selective 1st generation beta antagonists |
| What are ATENOLOL (TENORMIN) Acebutol Bisoprolol Esmolol Metoprolol | B1 selective 2nd generation antagonists |
| what are Carvedilol Labetalol | non-selective 3rd generation beta antagonists against B, and A1 receptors |
| What are Celiprolol Nebiprolol | B1 selective antagonist |
| What are the clinical uses of beta receptor antagonists (beta blockers) | Used in cardiovascular to treat -angina pectoris -myocardial infarction -arrhythmias -CHF -Hypertension Also used in -glaucoma -thyrotoxicosis -anxiety to control somatic symptoms -migrane prophylaxis |
| What are the clincal uses of propranolol a non selective 1st generation Beta antagonist | treatment of essential hypertension exercise induced angina arrythmias CHF myocardial infarction thyrotoixosis migrane prophylaxis |
| What is the MOA of Propranolol | lowers B/P in hypertensive patient blocks sympathetic activation of the heart, Reducing after load and CO, prolonged use can reduce TPR -Blocks renin release decreasing Angiotensin II formation |
| What is the clincal use of Timolol (betaoptic) a 1st geneartion non selective beta antagonist | Treatment of open angle glaucoma |
| What is the MOA of Timolol (betaoptic) a 1st geneartion non selective beta antagonist | reduces IOP by decreasing aqueous humor production by the ciliary body |
| What are the S/E of using a non-selective beta blocker | Arrhythmia, Bronchoconstriction (contra indicated in asthmatics) and sexual dysfunction |
| What are third generation beta antagonists | Beta blockers with additional effects -anti-oxidant effect -antiproliferative effect -membrane stabilizing properties -B2 agonist properties -A1 blockers 3rd generation has decrease in morbidity and mortality |
| What type of action do these drugs have Amphetamine Methamphetamine (DESOXYN) Dextroamphetamine (DEXEDRINE) Methylphenidate (RITALIN) | INDIRECT ACTING SYMPATHOMIMETICS |
| What is the action and MOA of amphetamines as an INDIRECT ACTING SYMPATHOMIMETICS | increases release of dopamine and biogenic amines MOA- inhibits dopamine vesicular transport, inhibiths uptake inhibits MAO (monoamine oxidase) |
| What are the clinical uses of Amphetamines | Effective orally can cross BBB to help treat Narcolepsy, ADHD, ADD and is an appetite suppressant |
| What type of drug is ephedrine | MIXED ACTING SYMPATHOMIMETICS Agonist at all adrenergic receptors Increases release of DA, NE Effective orally and crosses BBB Potent CNS stimulant |
| Agonist at all adrenergic receptors Increases release of DA, NE Effective orally and crosses BBB Potent CNS stimulant | Ephedrine |
| What are the S/E of sympathomimetics | Arhythmia, Headache, Hyperactivity, Insomnia, Nausea, tremors |
| What are MAO inhibitors and COMT inhibitors | drugs taht inhibit catecholamine metabolism increasing their duration of action |
| what are Phenelzine Tranylcypromine Selegiline | MAO inhibitors |
| what are Entacapone Tolcapone | COMT inhibitors |
| Review Slide 60 | Review slide 60 |
Created by:
smaxsmith
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