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HiralOT_ADRENERGIC DRUGS Cheat Sheet by

pharmacology

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.
 

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)
 
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 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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