Beta 1 Selective AgonistsLocated at | Myocardium | Stimulation results in | Increased Heart rate and increased force of myocardial contraction (Increased Cardiac output) | USED FOR | To increase cardiac output in emergency situations such as CVS shock or to treat complications in Cardiac Surgery. | also USED FOR | To increase cardiac function in the short-term treatment of certain type of heart disease, - heart failure | Dobutamine (Dobutrex) | Use: Short term mx of Cardiac decompensation that occurs during heart disease or heart surgery. How: Increase force of cardiac contraction. Adm: IV pump infusion (to stable plasma levels) | Dopamine (Intropin) | directly stimulates Beta 1. Low DOSE: cause peripheral vasodilatation. Adm: IV drip to maintain stable plasma levels | ADVERSE Effects | Chest pain, difficulty in breathing |
Beta 2 Selective AgonistsLocation | on bronchiole smooth muscle | How | Stimulated Beta 2 --> mediates relaxation of bronchioles | Treat | Bronchospasm associated with respiratory ailments such as asthama, bronchitis, emphysema. Treats ALSO Cardiac Arrythmias or heart failure | Another LOCATION | Uterine Muscle (When stimulated-->cause inhibition or relaxation of the uterus) | Beta 2 Selective Bronchodialators | Albuterol (Provventil, Ventolin), Metaproterenol (Alupent,), Pirbuterol (Maxair), Salmeterol (Servent), and Terbutaline (Brethaire, bricanyl). | what it causes | Bronchodilatation at pulmonary smooth muscles - Asthma. | Isoproterenol (Isuprel) | can be the same but: less beta 2 selective and affects beta 1 receptor too. | Adm | Oral inhalation so that affects on the bronchial membranes. | Adverse Effect | nervousness, restlessness, trembling. sometimes fatal asthamatic attaacks. | When used to treat premature labor, | Terbutaline - increase in maternal heart rate and systolic blood pressure, as well as maternal pulmonary edema. Sometimes fatal to mother. |
| | Adrenergic DrugsAdrenergic | Refers physiological responses related to adrenaline and noradrenaline | Other names | Adrenaline and NorAdrenalin = Epinephrine and NonEpinephrine | Adrenergic Drugs | Stimulate activity in tissues that respond to Epi and NorEpi (Adrenergic agonists) OR inhibit epinephrine and norepinephrine influence (adrenergic antagonists) | From where they release? | Adrenal gland and reach to Heart, Kidneys, and various other tissues and organs via systemic circulation. | Where it is found | Junction between sympathetic postganglionic neurons and peripheral tissues | Adrenergic agonists | Sympathomimetic | Adrenergic antagonists | sypatholytic |
Subclassification of Adrenergic DrugsAdrenergic receptors can be divided into two | Alpha and Beta receptors | Five receptor subtypes | Alph 1 (a, b, d) 2 (a, b, c) beta 1,2,3, | Alpha 1 or alpha 2 | Located at specific tissues throughout the body--> the responsed depend upon interaction between that receptor andthe reseptive tissue | Agonist | Increase or mimic the receptor mediated response | Antagonist | decrease the receptor mediated resonce | Epinephrine drug | affects alpha and beta receptors Equally | Receptor selectivity |
MIX ALPHA AND BETAAmphatamines | Drugs:Amphetamine (generic), dextroamphetamine (Dexedrine) and methamphatamine (Desoxyn) | Increase Norepi release and decrease NorEpi reuptake and breakdown at adrenergic synapses - so Increase activity at synapses with Norepi sesitive receptors - Alpha 1,2 and Beta1) | | Used to treat attention-deficit disorder in children, to increase mental alertness in adults with narcolepsy. | The use to suppress appetite or to combat normal sleepiness is discourage- as they have high potential of abuse | Ephendrine (Generic) | Stimulate Alpha 1, 2 and beta 1 and also stimulate the same by increasing release of norepi at synapses | Use: Primarily for Alpha 1 effects: treat hypotension. | | IV injection | ALSO a nasal decongenstant - stimulate alpha 1: combined with other agents (antitussives, antihistamines) to form cough and cold products | | As Bronchodilator | Narcolepsy treatment | Epinphrine (Adrenalin, Bronkaid Mist, Primatene Mist, ) | All receptors are stimulated. | Antiasthmatic inhalation products. - primary stimulate B2 bronchii. | | Effect of Alpha 1 vascular | vasoconstirction and control of bleeding during minor surgical procedures (sutures). Prolongs effects of the anasthetics | | B1 effect on heart | reestablish normal cardiac rhythm during cardiac arrest. | | Drug of choice in Anaphylactic shock | hypersensitive allergic reaction marked by CVS collapse (decreased cardiac output, hypotension) and severe bronchoconstriction. | why | Becase ability to | Stimulate heart (b1), vasoconstriction periphery (alpha 1) and Dilate bronchi (beta2). | Metaraminol (aramine) | act like Epinephrine | Directly stimulates alpha 1, 2 and beta1 | | Treat | shock or general anasthesia | NorEpiNephrine (Levophed) | Stimulates: Alpha 1, 2 and Beta 1. | displays little agonistic activity toward beta2. | | Adm IV injection | Treat: Hypotension during shock or general anasthesia. | Adverse Effect | Nervousness, restlessness, anxiety. | Prolonged use Causes- hypertension, arrhythmias, cardiac arrest. | | | Prolonged Use in inhalation: Cause bronchial irritation. |
| | ALPHA 1 SELECTIVE AGONISTSAlpha 1 or alpha 2 | Contraction and VasoConstriction : Increase BP | Mephentermine (Wyamine) | Maintain/restore BP during hypotensive episodes. Administered: IV or IM injections. | Methoxamine(Vasoxyl) | Increase and maintain BP in severe hypotension- during general anesthesia and spinal anesthesia. Treats: Paroxymal sypraventricular tachycardia by causing peripheral vasoconstriction, activation of baroreceptor reflex. Adm : IV injection | Midodrine (ProAmatine) | Treat: orthostatic hypotension Adm: Orally Also: treat hypotension in patients who go under dialysis, offset the hypotensive effects of psychotropic drugs like antipsychotic medications | Oxymetazoline (Afrin, OcuClear, Many others) | Adm: naslal drops and nasal sprays. Treat: Decrease nasal congestion and decrease redness and minor eye irritation | Phenylephrine (Neo-Synephrine, Others) | Treat: hypotension, treat certain episodes of supraventricular tachycardia. Adm: Orally a lso or nasal spray, or topically as eye drops. | Pseudoephedrine (Drixoral, Sudafed, etc) | Adm: Orally - relieve cold symptoms | Xylometazoline (Otrivin) | nasal spray to decrease congestion during cold and alergies. | Adverse Effect: | increased BP, headache, abnormally slow heart rate, sometimes chest pain, difficulty in breathing, feelings of nervousness |
ALHA 2 SELECTIVE AGONISTSPrimary use | Hypertension, spasticity.. | How | Drug stimulate alpha-2 receptors located at brain and brainstem --> cebtral alpha2 exert an inhibitory effect on sympathetic discharge from the vasomotor center in the brainstem ---> diminished sympathetic discharge results in decreased BP. | Also effective on Spinal cord | Stimulation of Alpha 2 --> causes interneuron inhibition and a subsequent decrease in excitability of motor neurons supplied by interneurons. USE TO normalize the neuronal activity in Spasticity | Brimonidine (Alphagan) | Adm: local to eye to treat glaucoma. (Decreases vitreous humor production and increasing drainage of vitreous humor from the eye) | Clonidine (Catapres, Duraclon) | Antihypertensive and analgesic, It does not effect ALONE. so given with PRAZOSIN (Minipress - alpha antagonists). also useful to treat severe pain in cancer. | Guanabenz (Wytensin) | decrease BP (same as Clonidine) | Guanfacine (Tenex) | similar to Guanabenz | Methyldopa (Aldomet) | Antihypertensive. | Tizanidine (Zanaflex) | To treat spasticity. Similar to Clonidine but has fewer vasomotor effects and less likey to cause hypotension and other CVS problems. | Adverse Effects | Hypotension, dizziness, drowsiness, dry mouth. Difficulty in breathing, slow heart rate, persistent fainting - overdose of drugs. |
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