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