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63 Cards in this Set
- Front
- Back
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To prevent or reverse the effect of a result of excessive amount of the alpha-stimulant norepinephrine or levarterenol (Levophed) in the fingers, you can give an ...., like ...
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alpha-antagonist (blocker)
Phentolamine (Regitine) |
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alpha agonist increases ...
beta-1 provides ... stimulation beta-2 provides ... |
blood pressure
cardiac bronchodilation |
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Pseudoephedrine restrictions:
The U.S. DEA (and most states) has asked pharmacies and stores to limit the OTC sale of ephedrine and pseudoephedrine since these substances are used in the clandestine manufacture of ... -Stores should also be suspicious when a person purchases large amounts of isopropyl alcohol, iodine, muriatic acid and anhydrous ammonia, also used to make ... |
methamphetamine (“meth”)
meth |
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Uses of Alpha-only and Mixed Agonists:
... reactions (Anaphylaxis) Nasal and sinus ... -Decreases volume of blood in the sinus vessels (sinusoids), thereby reducing blood supply to mucosa, which decreases mucosal edema and improves nasal patency. Broncho... ... shock and ... shock |
Allergic
decongestant dilation Cardiogenic, hypotensive |
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Oral Sympathomimetics linked with stroke:
... was on the market for >50 years, with billions of doses consumed, but was associated with problems, particularly when used in large doses (75 mg) in products such as Dexatrim. It was removed from most products in late 2000 due to safety concerns based primarily on a study at Yale University, published in NEJM, suggesting that it increased some user’s risk of stroke. -Since they are so closely related, there is concern that pseudoephedrine and phenylephrine potentially could cause the same type problems. |
Phenylpropanolamine (PPA)
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Rebound Nasal Congestion from Topical Decongestants (Rhinitis Medicamentosa):
This occurs primarily following ... of intranasal decongestants and cocaine. -It occasionally occurs with the use of systemic decongestants. It should be treated with intranasal .... -A short course of oral ... is sometimes necessary to permit discontinuation of topical decongestants. |
overuse
corticosteroids corticosteroids |
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In January 2008, the FDA officially declared that infants and toddlers under ... years old should not be given over-the-counter cough and cold medicines because they are too dangerous for that age group.
Honey is recommended instead, except for children under 12 months. |
2
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Beta stimulants or agonist (Betamimetic) history:
In 1947, isoproterenol was approved and for the next 25 years, this drug and theophylline were the major bronchodilators used in clinical practice. Subsequent to isoproterenol, metaproterenol was released in 1973, followed, over the next decade, by additional beta-agonists, each with increasing specificity for beta-2-receptors. The dominant beta-agonist bronchodilator in use today, ..., was approved in 1981. ..., released in 1994 has yet a longer duration of action than albuterol. |
albuterol
Salmeterol |
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ß-only stimulants or agonist: MOA
Stimulation of ß-receptors leads to the activation of ... and to an increase in the intracellular concentration of .... |
adenylcyclase
cyclic AMP |
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ß-only stimulants or agonist: Effects
In addition to ... effects, these agents produce: ... effects from their actions on the beta-2 (lungs) receptors (chronotropic) and beta-1 (heart) receptors (chronotropic and inotropic). Excessive stimulation can lead to arrhythmias, hypertension, palpitations, and tachycardia. |
bronchodilatory
Cardiostimulatory |
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ß-only stimulants or agonist: Effects
Stimulation of beta-2 receptors in skeletal muscle results in ... and increased in strength of contraction while stimulation of beta-2 receptors in uterine smooth muscle causes ... (the delaying or halting of labor). Beta-2 stimulation activates Na+/K+/ATPase causing gluconeogenesis and increases ... secretion. These effects can contribute to ... (low concentration of K+ in blood) by causing an intracellular shift of potassium. Beta-2 stimulation can produce a metabolic lactic acidemia. |
tremors
tocolysis insulin hypokalemia |
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ß-only stimulants or agonist: Uses
... for asthma and COPD (ß2) ... stimulant (ß1) ... (uterine relaxant) (ß2) -Primarily terbutaline (Brethine®), but this is “off-label” |
Bronchodilation
Cardiac Tocolytic |
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Some agents are “selective” or “preferential” agonists for ß1 or ß2.
However, even “selective” agents are not 100% selective—there is some override, especially in higher doses. For ß-blockers, there are only ... selective blockers, since there would be no therapeutic application for ... selective blockers. |
ß1
ß2 |
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Long-Acting Selective ß2 Agonist: Warnings
All LABAs are required to have a warning stating that the drugs could increase the chances of ... that could result in death and should only be used after other medicines fail to control asthma. This includes Salmeterol (Serevent®), Formoterol (Foradil) and Arformoterol (Brovana®) |
severe asthma episodes
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ß-only Agonist: Adverse Effects :
Cardiovascular side effects associated with ... stimulation can be serious and include: -Palpitations -Tachycardia -Hypertension -Arrhythmias |
beta-1
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ß-only Agonist: Adverse Effects:
Inhaled agents can cause local ... effects include cough, wheezing, dyspnea, bronchospasm, throat dryness or irritation, and pharyngitis. ... has a high incidence of respiratory side effects (e.g. upper respiratory tract infections, nasopharyngitis) compared to the other beta-2 agonists. |
respiratory
Salmeterol |
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ß-only Agonist: Adverse Effects:
Beta-2 activity in the skeletal muscle can produce .... Beta-2 agonists also cause ... which can subsequently cause dizziness, headache, flushing, and sweating. |
tremors
vasodilation |
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ß-only Agonist: Adverse Effects:
... side effects include shakiness, nervousness, tension, excitement, and insomnia. Other effects include unusual or bad taste, anorexia, hypokalemia, lactic acidemia, and gluconeogenesis. |
CNS
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Alpha-blockers: Uses
Diagnosis and pre-op management of .... (tumor of adrenal gland) -Administer Regitine® and watch for a dramatic ↓ in blood pressure To reverse the ... effects of injected sympathomimetics (e.g., epinephrine, Levophed®, dopamine) Hypertension ... (BPH) |
pheochromocytoma
vasoconstrictive Benign Prostatic Hyperplasia |
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MOA of Alpha-blockers:
Unlike phentolamine and phenoxybenzamine, doxazosin, prazosin, terazosin, alfuzosin and tamsulosin are selective for the ... receptor. Because of this selectivity, reflex tachycardia and attenuation of the hypotensive effect are less of a problem than with either phentolamine or phenoxybenzamine. ... receptors are involved in contraction of smooth muscle and are abundant in the prostate, prostatic capsule, prostatic urethra, and bladder neck. |
alpha-1
Alpha-1 |
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Adverse Reactions of Alpha-blockers:
... is the major effect of alpha-blockade and is dose-related. -Sometimes called “...”, it occurs frequently with prazosin, terazosin and doxazosin (9-10%). Alfuzosin and tamsulosin have a ... incidence of orthostatic hypotension. |
Orthostatic hypotension
first-dose effect low |
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Other adverse effects associated with ... effects of alpha-blockers include:
-Reflex dizziness -Sinus tachycardia (angina, palpitations) -Syncope -Vertigo |
hypotensive
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all beta-blockers end in ...
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-olol
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ace inhibitors end in ...
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-pril
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It is increasingly being recognized that administration of beta-blockers following ... exerts a beneficial effect on mortality.
Beta-blockers have been beneficial for both primary and secondary ... prophylaxis to prevent sudden death and also are beneficial for the acute treatment of ... |
myocardial infarction
myocardial infarction myocardial infarction |
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Beta-adrenergic Blockers: Classification
... agents with or without intrinsic sympathomimetic activity (ISA) or partial agonist activity (PAA) ... (e.g., beta1-selective) agents with or without ISA/PAA ... (alpha- and beta-antagonist) agents. |
Nonselective
Cardioselective Dual-acting |
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Beta-adrenergic Blockers: Classification
Another distinction can be made with respect to lipophilicity of the beta-blockers. The more lipophilic drugs tend to be metabolized to a ... extent, to exhibit ... serum concentration variability, and to have a ... duration of activity. |
greater
greater shorter |
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There is some possibility that lipid-soluble beta-blockers may be more effective in prevention of ... following myocardial infarction.
Because the more ...-soluble members of the class appear to be more effective for this use, a central mechanism of action is proposed. ... (water-soluble) and ... (lipid-soluble) are approved by the FDA for early and late adjunctive treatment of acute myocardial infarction. |
sudden cardiac death
lipid Atenolol metoprolol |
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Mechanism of Beta-blockers:
In general, all beta-adrenergic antagonists compete with adrenergic neurotransmitters (i.e., catecholamines) for binding at ... receptor sites. These drugs block sympathetic stimulation mediated by ...-adrenergic receptors in the heart and vascular smooth muscle. |
sympathetic
beta-1 |
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Mechanism of Beta-blockers:
Blockade of beta-1-receptors ... both resting and exercise heart rate and cardiac output, ... both systolic and diastolic blood pressure, and ... the reflex response to orthostatic hypotension. |
decreases
decreases inhibits |
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Mechanism of Beta-blockers:
The fall in cardiac output induced by beta-1 antagonism is often countered by a moderate reflex increase in peripheral vascular resistance that can be magnified by ... blockade (unopposed ... stimulation). As a result, ... beta-blocking agents can produce a more modest decrease in diastolic blood pressure compared with selective beta-1 antagonists. |
beta-2
alpha nonselective |
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Mechanism of Beta-blockers:
In addition, nonselective agents can competitively block beta-2-adrenergic responses in the bronchial muscles, potentially inducing .... |
bronchospasm
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Uses of Beta-blockers: Hypertension
Therapeutic actions of beta-blockers in the treatment of hypertension include: -a negative ... (HR) effect that decreases heart rate at rest and after exercise -a negative ... (outflow) effect -reduction of sympathetic outflow from the CNS -suppression of renin release from the kidneys. Thus, beta-blockers affect blood pressure via multiple mechanisms. |
chronotropic
inotropic |
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Uses of Beta-blockers:
Chronic Stable Angina The reduction in myocardial oxygen demand induced by these agents ... the frequency of anginal attacks, ... nitrate requirements, and ... exercise tolerance. Other postulated anti-anginal actions include: -an ... in oxygen delivery to tissues as a result of beta-receptor antagonist's lowering of hemoglobin's affinity for oxygen -reduction of platelet aggregation is postulated to be related to interference with calcium ion flux |
decreases
decreases increases increase |
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A critical result of beta blockade is a reduction in ....
Beta-blockers can limit the severity and recurrence of infarction, as well as a decrease in mortality secondary to myocardial infarction. |
myocardial ischemia
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Although beta blockade is most beneficial when initiated within the first few days following acute ..., especially in the highest risk subgroup of patients, relative reductions in infarct size secondary to the use of beta-blockers can approach 10-30% per year.
As a result, beta-blockers should be considered ... for secondary prevention of reinfarction and reduction of late mortality in all patients who do not have a clear contraindication (asthmatic or diabetic) to beta blockade. |
myocardial infarction
standard therapy |
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In addition to a decrease in myocardial oxygen demand, beta-blockers also possess ... properties at the nodal level of pacemaker control.
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antiarrhythmic
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Beta-blockers have very little effects on thyroid hormone, but do help control the ... of hyperthyroidism
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symptoms
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Beta-blockade can attenuate somatic symptoms of ... such as palpitations and tremor, but it is less effective in controlling psychologic components, such as intense fear.
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anxiety
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Uses of Beta-blockers:
... of Migraine Headache Beta-blockers interfere with arterial dilation, inhibit renin secretion, and block catecholamine-induced lipolysis. Blocking lipolysis decreases arachidonic acid synthesis and subsequent prostaglandin production. Inhibition of platelet aggregation is secondary to a decrease in prostaglandins and blockade of catecholamine-induced platelet adhesion. Other actions include increased oxygen delivery to tissues and prevention of coagulation during epinephrine release. |
Prevention
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Uses of Beta-blockers:
Ophthalmic for Glaucoma Ophthalmic beta-blockers interfere with the production of aqueous humor via ... of adrenergically driven processes within the ciliary processes. As a result of their actions, IOP is reduced in patients with either elevated or normal IOP. This reduction occurs irrespective of the presence of glaucoma. Decreased aqueous humor may also be responsible for the ocular antihypertensive effects. Visual acuity, pupil size, and accommodation ... appear to be affected by beta-blockade. |
inhibition
do not |
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Adverse Effects of Beta-blockers :
The adverse effects of beta-blockers usually occur at the ... of therapy and diminish over time. Most adverse reactions of beta-blockers are extensions of their therapeutic effects. The role that the characteristics of cardioselectivity and ISA of beta-blockers play in these effects are more controversial. |
onset
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Adverse Effects of Beta-blockers :
Bradycardia and hypotension occur often, but are rarely serious and can be reversed with IV ..., if necessary. AV block, secondary to depressed conduction at the AV node, might necessitate sympathomimetic and/or pressor therapy or the use of a temporary pacemaker. |
atropine
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Adverse Effects of Beta-blockers :
Adverse CNS effects include dizziness, ..., and depression. -Although much less common with hydrophilic beta-blockers, CNS depression can occur, resulting in mental disorders, fatigue, and, in some cases, vivid dreams. Diarrhea and nausea/vomiting are the most common GI adverse effects. |
fatigue
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Adverse Effects of Beta-blockers :
Bronchospasm and dyspnea are more likely to occur with ... beta-blockers or with high doses of ... agents because the beta selectivity of the drug is lost. Patients with preexisting bronchospastic disease are at ... risk. |
nonselective
cardioselective greater |
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Adverse Effects of Beta-blockers :
Both hypoglycemia and hyperglycemia can occur. Beta-blockers can interfere with glycogenolysis to cause hyperglycemia and can also mask signs of hypoglycemia. Beta-blockers should be used cautiously in brittle .... |
diabetics
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Adverse Effects of Beta-blockers :
Do not ... stop therapy. The myocardium is sensitized to the ß-blockade and may be "super-reactive" to sympathetic stimulation. |
abruptly
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Adverse Effects of Beta-blockers :
Beta-blockers have little effect on total cholesterol and LDL, but have been shown to ... triglycerides and ... HDL. |
increase
decrease |
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Adverse reactions from ophthalmic beta-blockers are usually limited to their ocular effects, such as transient burning, stinging, and blurred vision however, these preparations can be absorbed causing ... adverse reactions, similar to oral or parenteral beta-blockers.
Ophthalmic betaxolol (Betoptic®) appears to cause less systemic effects compared to ophthalmic timolol (Timoptic®) and levobunolol (Betagan®). |
systemic
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Parasympathomimetic (Cholinergic or Muscarinic) Agonists and
Acetylcholinesterase Inhibitors: Acetylcholine functions as a neurotransmitter in many locations throughout the body. Cholinergic receptors have been categorized according to the actions of the selective cholinergic agonists ... and .... |
muscarine and nicotine
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Parasympathomimetic (Cholinergic or Muscarinic) Agonists and
Acetylcholinesterase Inhibitors: ... cholinergic receptors are located on smooth muscle, on secretory glands, in the heart, and throughout the CNS. Both muscarinic and nicotinic cholinergic receptors can be found in cortical and subcortical areas of the CNS, while ganglionic receptors are predominantly .... |
Muscarinic
nicotinic |
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Indirect Direct-Acting Parasympathomimetics:
... - Acetylcholinesterase inhibitors used as insecticides -... is antidotal |
Organophosphates
Atropine |
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Uses of Indirect Direct-Acting Parasympathomimetics:
Neurological diseases such as ... and myasthenia gravis ...—due to miotic effect ... associated with Sjögren’s syndrome To stimulate genitourinary tract in urinary retention and gastrointestinal tract |
Alzheimer's
Glaucoma Dry mouth |
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Side Effects of Indirect Direct-Acting Parasympathomimetics:
Abdominal cramping and diarrhea (contraindicated in ...) ... secretions (perspiration, saliva, etc.) Myosis |
ulcers
Increased |
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Anticholinergic Drugs (Parasympatholytics or Antimuscarinic):
All anticholinergic drugs interfere with the binding of acetylcholine at its .... The actions of the various anticholinergic drugs are a result of the specific receptor subtype affected, which, in turn, is determined by components of the drug's chemical structure. |
receptor
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Anticholinergic Drugs (Parasympatholytics or Antimuscarinic):
Drugs that have anticholinergic effects are derived from natural sources (...) such as the belladonna plant (Atropa belladonna or “Deadly Night Shade”) or are manufactured synthetically. Study of atropine's actions began in the 1830s. Many antimuscarinic anticholinergic compounds were made available in the 1950s and were the mainstay of therapy in ... disease until the release of cimetidine (Tagamet®) in 1977. |
alkaloids
peptic ulcer |
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Anticholinergic Drugs (Parasympatholytics or Antimuscarinic):
Nicotinic receptors are located within CNS ganglia and spinal synapses, and at the neuromuscular junction. Thus, ...- and succinylcholine-like neuromuscular blocking agents can also be considered "anticholinergics." |
curare
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Anticholinergic Drugs (Parasympatholytics or Antimuscarinic):
Several other classes of drugs also exhibit anticholinergic properties: -... (Traditional antihistamines; 2nd generation or “low-sedating” antihistamines do not have anticholinergic properties) -Phenothiazines -Tricyclic antidepressants -Carbamazepine |
H-1 blockers
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Uses of Anticholinergic Drugs:
Atropine and glycopyrrolate are often used prior to surgery to reduce ... that may be aspirated and also to prevent excessive vagal stimulation (vaso-vagal reflex) causing bradycardia, hypotension and cardiac arrest. They also can be used for “...” in patients with cerebral palsy or other disabilities. |
secretions
drooling |
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Uses of anticholinergic drugs:
Cyclopentolate and tropicamide are preferred ophthalmologic agents because of their relatively ... duration of action. When used to dilate pupils for optical examinations, anticholinergics cause both: -... is dilation of the pupil; ... is paralysis of the ability for “accommodation” or focusing mechanism in the eye. Adrenergic agents cause only ..., not .... |
short
Mydriasis cycloplegia mydriasis cycloplegia |
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Uses of Anticholinergic Drugs:
For many years, it was thought that atropine-like drugs were effective in the treatment of asthma. -In the 1950s there was an atropine containing cigarette called Asthmador® that was marketed to treat asthma. Then it was thought that these drugs were to be avoided in the treatment of asthma. Now, it has since been shown that antimuscarinic anticholinergics are indeed ... bronchodilators. |
effective
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Side Effects of Anticholinergic Drugs:
Adverse reactions to anticholinergic drugs are classic. Clever phrases are used by many in an attempt to remember and explain them: “...” are several that illustrate hyperthermia secondary to decreased sweating; mydriasis and cycloplegia; and xerostomia, respectively. |
hot as a hare, blind as a bat, dry as a bone
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Side Effects of Anticholinergic Drugs:
Tachycardia Constipation Urinary retention -Especially important in older male patients Dry mouth (...) Blurred vision -Due to ..., not ...—anticholinergics cause both, but mydriasis and cycloplegia; blurring of vision is related to ...) Increased body temperature (flushing) Central effects (confusion, amnesia, hallucinations) |
xerostomia
cycloplegia mydriasis cycloplegia |
