Beta 1 Selective Agonists
Located 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 Agonists
Location |
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. |
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Adrenergic Drugs
Adrenergic |
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 Drugs
Adrenergic 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 BETA
Amphatamines |
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) |
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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 |
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As Bronchodilator |
Narcolepsy treatment |
Epinphrine (Adrenalin, Bronkaid Mist, Primatene Mist, ) |
All receptors are stimulated. |
Antiasthmatic inhalation products. - primary stimulate B2 bronchii. |
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Effect of Alpha 1 vascular |
vasoconstirction and control of bleeding during minor surgical procedures (sutures). Prolongs effects of the anasthetics |
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B1 effect on heart |
reestablish normal cardiac rhythm during cardiac arrest. |
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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. |
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Prolonged Use in inhalation: Cause bronchial irritation. |
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ALPHA 1 SELECTIVE AGONISTS
Alpha 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 AGONISTS
Primary 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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