Term
| receptors that epi acts on and affinities? |
|
Definition
| acts on ALL adrenergic receptors with greatest affinity for B2 >B1> A |
|
|
Term
| receptors that NE acts on and their affinities? |
|
Definition
doesn't act on B2
affinities alpha's > beta-1 |
|
|
Term
| receptors that isoprotenolol binds to? |
|
Definition
|
|
Term
| what adrenergic receptors does dopamine bind to? |
|
Definition
| beta-1 and dopamine receptors D1 and D2 |
|
|
Term
| what receptors does dobutamine bind to? |
|
Definition
|
|
Term
| actions of alpha-1 activation? 5 things |
|
Definition
1. vasoconstriction
2. increase TPR
3. increase BP
4. mydriasis
5. contract bladder sphincter and trigone |
|
|
Term
| actions of alpha-2 activation? 3 things |
|
Definition
inhibit Ach release
inhibit NE release
inhibit insuling secretion |
|
|
Term
| actions of beta-1 activation? 3 things |
|
Definition
tachycardia
increase myocardial contractility
increase renin release |
|
|
Term
| actions of beta-2 activation? 5 things |
|
Definition
vasodilation
decreased TPR
bronchodilation
increase glycogenolysis
relax uterine smooth muscle |
|
|
Term
| vascular effects of NE and Epi on cutaneous vesels and skeletal muscles? |
|
Definition
cutaneous: only has alpha receptors. NE has high affinity --> vasoconstriction. Primary response to both epi and NE is vasoconstriction.
skeletal muscle: NE --> vasoconstriction and Epi --> vasodilation (therapeutic response) |
|
|
Term
| side effect of NE mediated increase in BP? |
|
Definition
| reflex bradycardia from strong baroreflex |
|
|
Term
|
Definition
used only in emergency situations
1. bronchospasm relief
2. cardiac resuscitation
3. reduce IOP
Used with anesthetic to increase effective time of local effect via vasoconstriction to maintain drug in tissues. |
|
|
Term
|
Definition
| hypertension, direct tachycardia, reflex bradycardia, arrythmias, tremor, and HYPERGLYCEMIA (beta-2 modulated release of glucagon). |
|
|
Term
| contraindications for use of Epi |
|
Definition
| hyperthyroidism, diabetes, and pt on beta blockers (unapposed alpha increase in TPR) |
|
|
Term
Dopamine cardiovascular effects?
Dopamine renal effects? |
|
Definition
| Beta-1 mediated increase in ionotropy Vascular D1 receptor mediated vasodilation Renal D1 receptor mediated inhibition of Na pump and Na/H exchanger in TAL. |
|
|
Term
| When is dopamine used clinically? |
|
Definition
| to improve cardiac and renal finction in pt with severe heart/renal failure. Only used after hypovolemia is treated. |
|
|
Term
| Dobutamine receptors and cardiovascular effects? |
|
Definition
selective for beta-1 receptors
ionotropic>chronotropic CVS effect w/o change in TPR. |
|
|
Term
| Clinical uses of dobutamine? |
|
Definition
| short term managment of decreased CO from surgery, CHF or MI |
|
|
Term
| Name the non-selective alpha agonist. |
|
Definition
|
|
Term
| what are the clinical uses of oxymetazoline? |
|
Definition
| Used as nasal decongestants. As an alpha agonists, it causes vasoconstriction of mucosal blood vessels and decreases mucous secretion. Can become desensitized. |
|
|
Term
| name the alpha-1 selective agonist |
|
Definition
|
|
Term
| Name 3 selective alpha-2 agonists. |
|
Definition
| Clonidine, apraclonidine, methyldopa |
|
|
Term
| clinical uses for phenylephrine? |
|
Definition
topical nasal decongestant
mydriatic agent** (produces mydriasis w/o loss of accomadation b/c no PNS interaction unlike atropine)
phenylephrine is contraindicated in narrow/closed angle glaucoma.
maintain BP during spinal anesthesia. |
|
|
Term
|
Definition
treat HTN Preparation for addiction withdrawal
binds to alpha 2 receptor on presynaptic terminal and inhibits release of NE to treat HTN
Can cross BBB to decrease sympathetic outflow from brainstem for withdrawal treatment
|
|
|
Term
| MOA for clonidine in HTN and withdrawal symptom relief |
|
Definition
being a selective alpha-2 agonist, it binds to the presynaptic A2 receptor inhibiting release of NE
can cross BBB to act on lower brainstem to decrease sympathetic outflow. |
|
|
Term
| abruptly stopping clonidine treatment will cause ___? |
|
Definition
|
|
Term
| apraclonidine (iopidine) is used clinically for what? |
|
Definition
| mostly used for treatment of OPEN angle glaucoma. Since it is a alpha-2 specific agonist --> decreases aqueous humor production w/o mydriasis (a1 mediated) |
|
|
Term
| name 2 beta-1 selective agonists |
|
Definition
|
|
Term
| name 3 beta-2 adrenergic receptor selective drugs |
|
Definition
| albuterol, salmeterol, ritodrine. |
|
|
Term
| Uses and MOA of salmeterol? |
|
Definition
| symptomatic relief of bronchospasm of COPD and nocturnal asthma. Has a long duration (12 hours) but with a slow onset so not used in acute attacks. |
|
|
Term
| clinical use of ritodrine and MOA? |
|
Definition
| specifically developed Beta-2 agonist to cause uterine relaxation to arrest premature labor |
|
|
Term
| beta-2 agonist side effects? 4 things |
|
Definition
| increase HR (???), tremor, decrease plasma K, increase blood glucose |
|
|
Term
| Name 2 non-selective alpha antagonists |
|
Definition
| phenoxybenzamine and phentolamine. |
|
|
Term
| name 2 alpha-1 selective antagonists |
|
Definition
|
|
Term
| Clinical use for non-selective alpha antagonists |
|
Definition
| phenoxybenzamine and phentolamine are used to treat pheochromocytoma via irreversible binding of alpha receptors --> decreased TPR and preload. |
|
|
Term
| side effects of phenoxybenzamine and phentolamine |
|
Definition
| reflex tachycardia, orthostatic hypertension, and tachycardia from increase NE due to presynaptic blockage of feedback A2 receptor. |
|
|
Term
| Clinical uses and MOA for prazosin |
|
Definition
HTN, CHF, and BPH
MOA: blocks alpha-1 receptor in arteries and veins to decrease TPR and preload. Can cross BBB to suppress sympathetic outflow from lower brainstem. |
|
|
Term
|
Definition
orthostatic hypotension and syncope especially upon first treatment. Limit with low initial dose and titrate up to therapeutic dose.
Retention of Na and water thus use w/ diuretic. |
|
|
Term
| Clinical use of tamsulosin |
|
Definition
| symptomatic relief of urinary symptoms of BPH by relaxing smooth muscle. pretty specific for a1 in the sphincter and trigone |
|
|
Term
| Name 3 non-selective (first generation) beta antagonists |
|
Definition
| proponanolol, timolol, sotalol |
|
|
Term
| Name 3 beta-1 selective (2nd gen) beta antagonists |
|
Definition
| atenolol (tenormin), esmolol, metoprolol |
|
|
Term
| Name 3 3rd generation beta antagonists? what makes a drug a 3rd gen beta antagonists? |
|
Definition
| Non-selective: labetalol and carvedilol B1 selective: nebivolol There are additional protective effects in order to be a 3rd gen. |
|
|
Term
| beta blockers with high lipophilicity |
|
Definition
| propanolol, timolol and metoprolol |
|
|
Term
name 4 membrane stabilizing beta blockers?
What does membrane stabilizing mean? |
|
Definition
propanolol, carvedilol, pindolol and acebutolol.
membrane stabilizing means hyperpolarizaion of the membrane via reduced Ca entry and open K channels. |
|
|
Term
| clinical uses of propanolol |
|
Definition
| treat essential HTN, exercise angina, arrythmias, CHF, MI, thyrotoxicosis, migraine prophylaxis (because of it lipophillicity) |
|
|
Term
|
Definition
| non selective beta blocker. with long term effects of decreasing renin release and formation of ANG II. |
|
|
Term
| timolol clinical uses and MOA |
|
Definition
| used to treat open angle glaucoma via block of non specific beta receptors and resulting decrease in aqueous humor production and decrease in IOP |
|
|
Term
| Pt presents with long history of moderate controlled asthma and has HTN. If you had to choose a beta blocker, which would it be? |
|
Definition
| atenolol because it is Beta-1 specificand won't interfere with asthma treatments (in a perfect world) |
|
|
Term
| side effects of beta blockers |
|
Definition
| rebound effects, asthma exacerbation, 1st and 2nd gen mask hypoglycemic symptoms (except sweating), sexual dysfunctions. |
|
|
Term
| advantage with 3rd gen beta blockers? |
|
Definition
| vasodilatory effects via B2 agonists, A1 blockers and NO mediated vasodilation, antioxidant effects, anti-proliferative effect on cardiac tissue |
|
|
Term
| clinical uses of lebetolol and MOA |
|
Definition
| reduce HR and contractility (B1 block) and reduce TPR (A1 block) and vasodilation (via B2 agonist) thus this is a 3rd gen blocker. |
|
|
Term
|
Definition
uses: HTN, CHF
MOA: reduce HR and contractility (B1 block)
decreae TPR (A1 block)
anti-oxidant properties |
|
|
Term
|
Definition
TREAT UNCOMPLICATED HTN.
High b1 selectivity and increase NO availability. |
|
|
Term
| name 4 amphetamines and identify what drug class they belong to |
|
Definition
they are indirect acting sympathomimetics
amphetamine
methamphetamine (desosxy)
dextroamphetamine (dexedrine)
methylphenidate (ritalin) |
|
|
Term
|
Definition
| increase release of dopamine via inhibition of uptake of biogenic amine NT's, and inhibit MAO. |
|
|
Term
| clinical uses for amphetamines? |
|
Definition
| narcolepsy, ADHD, ADD, appetite suppressant |
|
|
Term
| name the mixed acting sympathomimetic and its actions |
|
Definition
ephedrine
increases everything and can cross BBB. |
|
|
Term
Indirect acting sympatholytics (2)?
its use? |
|
Definition
1. methyldopa. used in pregnancy HTN.
2. Metyrosine. used in treatment of pheochromocytoma. |
|
|
Term
| use and 2 examples of monoamine oxidase inhibitors? |
|
Definition
| treats refractory depression. Phenelzine and Tranylcypromine and selegiline |
|
|
Term
|
Definition
| entacapone and tolcapone used in parkinsons. |
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