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Definition
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Definition
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Definition
| selective a1 blocker. accumulates in prostate |
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Definition
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Definition
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Term
| Phenoxybenzamine (Dibenzyline) |
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Definition
nonselective A blocker
Non-competitive inhibition. Action slow in onset but
irreversible. Only synthesis of new receptors
can restore α-adrenergic functions |
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Term
| Phentolamine (generic, OraVerse) |
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Definition
| nonselective alpha blocker (PheN) |
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Term
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Definition
| selective B agonists. B2 > B1. rescue inhalers. terbutaline= uterine relaxation. |
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Definition
| B1 agonist. increase Cardiac Output |
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Definition
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Definition
| combination A B antagonist |
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Term
ACTIONS AND USES AS RELATED
TO INHIBITON OF β1 RECEPTORS |
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Definition
By inhibiting cardiac β1 receptors, all β-blockers
can ↓ most sympathetically-supported cardiac
functions, e.g. heart rate, contractility,
automaticity and conduction.
By ↓ heart rate and contractility they can ↓
myocardial O2 deficit that causes angina in
patients with poor coronary O2 delivery (due to
coronary atherosclerosis). Thus, an
antianginal use.9
Also, by ↓ rate and contractility they can ↓
cardiac output which helps to lower arterial
pressure in hypertensive patients. A ↓ in renin
secretion by inhibiting β1 receptors in kidney JG
cells also contributes to the antihypertensive
effect.
By ↓ automaticity in potential cardiac
pacemaker cells they may help prevent a
variety of post-M.I. arrhythmias. By slowing
conduction velocity in the A-V node, they can
also treat supraventricular arrhythmias.
Also, by ↓ rate and contractility they can ↓
cardiac output which helps to lower arterial
pressure in hypertensive patients. A ↓ in renin
secretion by inhibiting β1 receptors in kidney JG
cells also contributes to the antihypertensive
effect.
By ↓ automaticity in potential cardiac
pacemaker cells they may help prevent a
variety of post-M.I. arrhythmias. By slowing
conduction velocity in the A-V node, they can
also treat supraventricular arrhythmias. |
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Term
ACTIONS AND USES AS RELATED
TO INHIBITON OF β2 RECEPTORS |
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Definition
By inhibiting β2 receptor-mediated facilitation of
aqueous humor production in the ciliary
epithelium in the eye, nonselective agents
(applied topically) can lower intraocular pressure
and are used to treat glaucoma. |
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Term
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Definition
| glaucoma. decrease eye pressure w/o LA action. |
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Term
| Non-Selective (α1 and α2) Blockers |
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Definition
1. PheNoxybenzamine (Dibenzyline)*
2. PheNtolamine (generic, OraVerse)* |
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Term
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Definition
1. PrazoSin (Minipress)*
2. TerazoSin (Hytrin)*
3. Doxazosin (Cardura)*
4. Tamsulosin (Flomax)*
5. Alfuzosin (Uroxatral)*
6. Silodosin (Rapaflo)* |
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Term
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Definition
| selective a1 blocker. mild to moderate hyper tension. relax smooth muscle. first dose phenomenon (Orthostatic hypotension with syncope) |
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Term
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Definition
Newer α1-receptor blockers.
almost identical to prazosin; However, half-lives are much longer; so may be better
compliance for long-term control of
conditions like chronic hypertension. |
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Term
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Definition
Both fairly selective for blocking the subtype A
alpha-1 receptor (α1A) which is the main
subtype in smooth muscle of the bladder neck
and prostate.
Thus, good drugs to treat BPH because more
specific with less frequent and/or less severe
systemic side effects than the other α1 blockers
described above. |
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Term
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Definition
| Accumulates in prostatic tissue. |
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Term
Suddenly standing upright after reclining in a dental
chair may cause orthostatic hypotensive symptoms when taking... |
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Definition
taking systemic doses of the alpha-1 receptor
blocking drugs prazosin, doxazosin or terazosin. |
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Term
| Peripherally-Acting Sympathetic Neuronal Blockers |
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Definition
decrease availability of the sympathetic transmitter (NE)
to its receptors.
– *Reserpine
– Guanethidine |
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Term
| Centrally-Acting Sympathetic Neuronal Blockers |
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Definition
stimulates CNS α2 adrenergic receptors, thus (amoung
other actions) indirectly reduces nerve traffic from central
sympathetic vasomotor centers to peripheral organs
(especially CV).
Hyper tension in prego
– * Methyldopa
– *Clonidine (Catapres)
– Guanabenz
– *Guanfacine (Tenex, Intuniv) |
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Term
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Definition
PAANI – Decreases uptake of DA and NE into storage
vesicles within sympathetic nerve endings, thereby
depleting the stored level of NE. In the CV system,
this reduces BP by decreasing both cardiac output
and peripheral arterial resistance. Thus, used to
treat hypertension. |
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Term
| Alpha-methyldopa (or just methyldopa) |
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Definition
Actions. Enzymes that convert Dopa to DA to
NE also convert this prodrug to alphamethylnorepinephrine which is then active as
an α2 adrenergic agonist in central vasomotor
centers, dampening outflow of sympathetic
nerve activity to peripheral CV tissues. As a
result, renal renin release decreases, heart
rate and cardiac output may be decreased
and peripheral resistance falls.
treats hypertension during pregnancy
"autoimmune" disorders not seen with
others |
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Term
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Definition
Like methydopa BUT
also available as a dermal patch for
smoother BP control, less severe side effects
(except for skin reaction).
Rebound hypertension with abrupt cessation of
the drug
Also used in treatment of withdrawal from
addictive drugs and treatment of ADHD,
PTSD, migraine and menopausal hot
flashes |
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Term
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Definition
"Intuniv" (ADHD) in children and adolescents.
Alpha-2 antihypertensive use (Tenex)
side effects similar to clonidine, though
slightly less sedation and less tendency
toward withdrawal (rebound) syndrome. |
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Term
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Definition
| Are bad. (Ganglionic lecture in a nutshell) |
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Term
| Inhibit release reaction (degranulation) |
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Definition
–
*cromolyn sodium and nedocromil sodium
–
agents that increase cyclic AMP (e.g. methylxanthines, β-agonists) stabilize mast cells even though that is not their primary effect.
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Corticosteroids |
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Term
Inhibit formation of generated autocoids via:
–
cyclooxygenase pathway (PGD2, PGE2, PGF2, TXB2)
–
lipoxygenase pathway |
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Definition
Zileuton (Ziflo) acts by inhibiting the lipooxygenase enzyme and decreasing the formation of leukotrienes.
In addition, Zafirlukast (Accolate) and *Monteleukast (Singulair) act by blocking leukotriene receptors |
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Term
Block receptors for autocoids or bronchoconstrictors
– |
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Definition
H1 antihistamines (limited effect on airways but can reduce symptoms at other sites)
–
Anticholinergics (Ipratropium and tiatropium) |
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Term
Bronchodilation by "physiologic antagonists"
– |
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Definition
β-adrenergic agonists (epinephrine, isoproterenol, terbutaline, salmeterol, etc...)
–
methylxanthines (theophylline, aminophylline). |
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Term
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Definition
| Omalizumab (Xolair) MAB against IgE |
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Term
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Definition
| Ipratopium, Atrovent and *Tiatropium, Spiriva) |
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Term
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Definition
Stimulates all α and β receptors with varying effects:
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↑ force and rate of cardiac contraction
–
peripheral vasodilation and/or vasoconstriction
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bronchodilation |
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Term
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Definition
Stimulates α and β1 receptors (but not β2)
Vasoconstriction with some reflex bradycardia.
Used as a pressor agent during surgery requiring spinal anesthesia and in treatment of some types of shock. |
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Term
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Definition
Phenylephrine
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selective stimulation of α1 raises BP much like NE but with potentially more reflex bradycardia than NE. [ Why? No opposition from SA nodal β1 ].
–
used to maintain diastolic and mean BP in neurogenic shock and during therapeutic spinal (and even general) anesthesia. Also, as a nasal decongestant, mydriatic agent and for hemorrhoids. Rarely, for SVTs.
Midodrine
–Used for orthostatic hypotensive symptoms. Also, urinary incontinence (investigational). |
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Term
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Definition
Indirect-acting Sympathomimetic Agent
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A good anesthetic! But also INHIBITS REUPTAKE OF NE at sympathetic nerve terminals thus leaving more transmitter (NE) available to whatever receptors are present [It does this in brain, too, where it also affects DA].
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By inhibiting reuptake of peripheral NE it constricts blood vessels at site of LOCAL injection, retarding its own loss from the site. Thus, still listed as a topical LOCAL anesthetic for mucous membranes AND for intubation of the trachea through the nose. |
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Term
| Pseudoephedrine (Sudafed) and Ephedrine |
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Definition
| Stimulate release of NE from sympathetic nerve endings independent of nerve action potentials; they may also stimulate adrenergic receptors directly. |
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Term
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Definition
| nonselective beta agonist. B1 + B2 >> all others |
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Term
| Methylxanthines (*Theophylline and *Aminophylline) |
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Definition
Asthma. Theo=Oral Amino=IV
cause bronchodilation and may also inhibit release of mediators from mast cells.
mechanism of action - current hypotheses are:
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inhibition of phosphodiesterase leading to increased cyclic adenosine monophosphate (c-AMP) in smooth muscle and mast cells
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interaction with adenosine receptors; the role of the purinergic nervous system in controlling bronchial tone is a subject of active investigation |
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Term
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Definition
lipoxygenase inhibitor
taken orally to reduce frequency and severity of attacks.
potential for elevation of liver enzymes and hepatotoxicity.
must be taken 4 x per day which makes it difficult to use. |
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Term
| Chronic Asthma Therapy (Common Tx) |
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Definition
| use a bronchodilator for acute attacks, as well as a stabilizing agent (ie. cromolyn) and an antiinflammatory steroid or a leukotriene modulator. |
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Term
| The standard therapeutic dose of morphine is: |
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Definition
| 10 mg SC or IM. This is the dose to which all other analgesic drugs are compared. |
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Term
| Hydromorphone (Dilaudid, Palladone) |
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Definition
| - similar to morphine but more potent |
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Term
| Oxycodone (Roxicodone, Percodan, OxyContin) - |
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Definition
| similar to both morphine and codeine, but used orally (usually in combinations with acetaminophen) for mild-moderate pain. OxyContin is a sustained release oral preparation for the management of severe chronic pain. |
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Term
| *Hydrocodone (Vicodin, Norco, and many others) - |
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Definition
| similar both to morphine and codeine; used orally for mild-moderate pain and as an antitussive; is currently one of the most widely prescribed opioids |
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Term
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Definition
synthetic drug
route of administration - oral and parenteral
1/10 the potency of morphine
reputed to have weaker effects on smooth muscle than morphine - less constipation and urine retention, although the evidence to support this is weak.
has been commonly used in obstetrics - may cause less respiratory depression in the newborn than morphine
relatively short acting 1-3 hours; not appropriate for chronic pain because of the buildup of an active metabolite (normeperidine) that can cause seizures.
falling into disfavor in many circles. |
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Term
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Definition
less euphoric and longer duration of action (12-24 hours) than heroin (4-6 hours) or morphine (4-6 hours)
used as an analgesic and in treating opioid addiction
dosing can be tricky and needs to be done carefully, with close monitoring of the patient.
–
Note: When used acutely as an analgesic, methadone has a duration of action of 4-6 hours. However, when used chronically (as in methadone maintenance for the treatment of opioid dependence, or for the management of chronic pain), it has a duration of action of 12-24 hours. |
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Term
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Definition
very potent mu agonist (about 100 x more potent than morphine)
given parenterally to supplement surgical anesthesia.
A transdermal preparation (Duragesic) is available for the management of chronic pain.
fentanyl plus droperidol (Innovar) can induce a state called neuroleptic analgesia (Conscious sedation). |
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Term
| *Pentazocine (Talwin; Talwin NX) |
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Definition
Mixed Agonist-Antagonist
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agonist effects are dominant - acts as an agonist at κ (kappa) receptors, but only as a partial agonist at μ (mu) receptors; it acts as a μ antagonist at high doses.
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less effective than morphine for severe pain
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sedation and respiratory depression are less than with morphine
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CNS stimulation and hallucinations are more common than with morphine
–
with chronic use, the potential for physical dependence is less than morphine, but still significant
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can precipitate withdrawal syndrome in opioid addicts
–
Talwin Nx is a preparation that contains petazocine and naloxone. The latter is included to reduce the potential for IV abuse. |
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Term
| Buprenorphine (Buprenex, Subutrex, Suboxone, Butrans)) |
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Definition
Mixed agonist-antagonist
mu receptor, possibly k
low abuse potential |
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Term
| *Naltrexone (Trexan, ReVia) |
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Definition
orally effective, long acting antagonist (24 hours)
used in "IMMUNIZING" addicts (ie. preventing the high produced by opioid agonists)
risk of hepatotoxicity is a serious drawback |
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Term
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Definition
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Term
Doxylamine* (Unisom)
*Promethazine (Phenergan)
*Hydroxyzine (Atarax; Vistaril) |
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Definition
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Term
*Diphenhydramine (Benadryl)
*Dimenhydrinate (Dramamine)
*Chlorpheniramine maleate (Chlor-Trimeton)
*Meclizine (Bonine) |
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Definition
| Moderately-Sedating Antihistamines |
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Term
*Cimetidine (Tagamet)
–
*Ranitidine (Zantac)
–
*Famotidine (Pepcid)
–
*Nizatidine (Axid) |
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Definition
| H2 antagonists (gastric H blockers) |
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