Term
|
Definition
Cholinomimetic (direct acting)
Use- post operative and neurogenic ileus & post-op urinary retention.
Mech - activate bowel and bladder smooth muscle.
Toxicity-SLUDGE |
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Term
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Definition
Cholinomimetic (Direct Acting), chiefly muscarinic
Non-ester so resists degradation by acetylcholinesterase. |
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Term
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Definition
Cholinomimetic (Direct Acting), chiefly muscarinic, tertiary amine.
Non-ester so resists degradation by acetylcholinesterase. Use-Glaucoma Mech-contraction of papillary sphincter & ciliary muscle, which allows flow of aqueous humor from ciliary epithelium. Tox-SLUDGE |
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Term
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Definition
Cholinomimetic (Direct Acting), chiefly muscarinic
Non-ester so resists degradation by acetylcholinesterase.
Use-dry mouth; aka xerostomia (Sjrogen's Syndrome or Radiation)
Mech-increases salivation
Tox-SLUDGE |
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Term
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Definition
Indirect Acting, Acetylcholinesterase Inhibitor
quaternary ammonium group
Use-post-operative & neurogenic ileus, post-op urinary retention, Myasthenia Gravis Mech-increase acetylcholine Tox-SLUDGE Edrophonium, which has a short acting so can be used to assess effective dosage of nestigmine. |
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Term
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Definition
| Indirect acting, Acetylcholinesterase Inhibitor Use-Myasthenia Gravis Mech-increase acetylcholine Tox-SLUDGE |
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Term
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Definition
Indirect acting, Acetylcholinesterase Inhibitor
Use-Myasthenia Gravis
Mech-increase acetylcholine
Tox-SLUDGE
Used to assess effective dosage of neostigmine due to it transient effect. |
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Term
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Definition
| Indirect acting, Acetylcholinesterase Inhibitor Use-Glaucoma Mech-increase acetylcholine Tox-SLUDGE |
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Term
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Definition
Indirect acting, Acetylcholinesterase Inhibitor
Use-Glaucoma
Mech-increase acetylcholine
Tox-SLUDGE |
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Term
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Definition
Indirect acting, Acetylcholinesterase Inhibitor
Use-Alzheimer
Mech-increase acetylcholine
Tox-SLUDGE |
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Term
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Definition
| aka PAM, reactivates acetylcholinesterase bound by organophosphate (Soman or Sarin) via displacement. PAM accepts the organophosphate. But this must be done before the organophosphate AGES. Once aging is complete the inhibition is irreversible. Sarin ages in 2 minutes. |
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Term
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Definition
Direct Acting, cholinomimetic, specific to nicotinic receptors.
tox-SLUDGE |
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Term
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Definition
| Acetylcholine induced vasodilation. Normally acetylcholine leads to vasoconstriction; however, Ach activates M3 receptors present on endothelial cells. Via Gq, calcium increases and leads to generation of NO (aka endothelial derived relaxation factor). NO acts on smooth muscle cells and leads to relaxation. |
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Term
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Definition
Cholinergic Receptor Inhibiting Drug; anti-muscarinic (effects parasympathetic innervation)
Found in plant, Atropa belladonna or deadly nightshade
Use-mydriasis (dilation of eye), cycloplegia (paralysis of ciliary muscle & loss of accommodation).
Tox- 1) Dry as a bone 2) blind as a bat 3) red as a beet 4) mad as a hatter
Sweat glands are sympathetic, but use cholinergic post-gang fibers. This can disrupt thermoregulation.
Emergency use for atropine-tx of poisoning with acetylcholinesterase inhibitors. Atropine can enter CNS. |
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Term
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Definition
Cholinergic Receptor Inhibiting Drug; anti-muscarinic (effects parasympathetic innervation)
Use-mydriasis & cycloplegia (Tertiary amine, can cross BBB).
Tox- 1) Dry as a bone 2) blind as a bat 3) red as a beet 4) mad as a hatter
Sweat glands are sympathetic, but use cholinergic post-gang fibers. This can disrupt thermoregulation.
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Term
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Definition
Cholinergic Receptor Inhibiting Drug; anti-muscarinic (effects parasympathetic innervation)
Use-prevents or reduces motion sickness
Tox- 1) Dry as a bone 2) blind as a bat 3) red as a beet 4) mad as a hatter
Sweat glands are sympathetic, but use cholinergic post-gang fibers. This can disrupt thermoregulation.
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Term
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Definition
Cholinergic Receptor Inhibiting Drug; anti-muscarinic (effects parasympathetic innervation)
Use-reduce transient hypermotility (Tertiary amine, can cross BBB).
Tox- 1) Dry as a bone 2) blind as a bat 3) red as a beet 4) mad as a hatter
Sweat glands are sympathetic, but use cholinergic post-gang fibers. This can disrupt thermoregulation.
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Term
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Definition
Cholinergic Receptor Inhibiting Drug; anti-muscarinic (effects parasympathetic innervation)
Use-tx transient cystitis, post-op bladder spasm or incontinence. (Tertiary amine, can cross BBB).
Tox- 1) Dry as a bone 2) blind as a bat 3) red as a beet 4) mad as a hatter
Sweat glands are sympathetic, but use cholinergic post-gang fibers. This can disrupt thermoregulation.
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Term
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Definition
Cholinergic Receptor Inhibiting Drug; anti-muscarinic (effects parasympathetic innervation)
Use-bronchodilation in asthma COPD (Quaternary amine, cannot cross BBB as well).
Tox- 1) Dry as a bone 2) blind as a bat 3) red as a beet 4) mad as a hatter
Sweat glands are sympathetic, but use cholinergic post-gang fibers. This can disrupt thermoregulation.
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Term
|
Definition
Cholinergic Receptor Inhibiting Drug; anti-muscarinic (effects parasympathetic innervation)
Use-bronchodilation in asthma COPD (Quaternary amine, cannot cross BBB as well).
Tox- 1) Dry as a bone 2) blind as a bat 3) red as a beet 4) mad as a hatter
Sweat glands are sympathetic, but use cholinergic post-gang fibers. This can disrupt thermoregulation.
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Term
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Definition
Cholinergic Receptor Inhibiting Drug; anti-muscarinic (effects parasympathetic innervation)
Use-tx manifestations of Parkinsons in CNS. Can cross BBB (tertiary amine).
Tox- 1) Dry as a bone 2) blind as a bat 3) red as a beet 4) mad as a hatter
Sweat glands are sympathetic, but use cholinergic post-gang fibers. This can disrupt thermoregulation. |
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Term
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Definition
Ganglionic Blocker, nicotinic receptor blocker (NN)
-does not cross BBB.
-used as antihypertensive. blood vessels receive chiefly vasoconstrictive fibers from sympathetic so blocking these leads to vasodilation. |
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Term
|
Definition
NMJ blocker, Nicotinic receptor blocker (NM)
non-depolarizing blocker, competitive inhibitor
use-flaccid paralysis, great for surgery.
affects can be overcome with acetylcholinesterase inhibitors.
Tox-respiratory paralysis and disturbance of autonomic function. |
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Term
|
Definition
NMJ blocker, Nicotinic receptor blocker (NM)
non-depolarizing blocker, competitive inhibitor
use-flaccid paralysis, great for surgery.
affects can be overcome with acetylcholinesterase inhibitors.
Tox-respiratory paralysis and disturbance of autonomic function. |
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Term
|
Definition
NMJ blocker, Nicotinic receptor blocker (NM)
Drug is an AGONIST!!! (depolarizing blocker - acts on nicotinic receptor and depolarizes, but prevents repolarization)
Use-muscle relaxation & flaccid paralysis, great for intubation because it is short acting (rapidly hydrolyzed by plasma acetylcholinesterase).
Tox-respiratory paralysis and disturbance of autonomic function. |
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Term
|
Definition
Degrades SNAP-25 preventing fusion of synaptic vesicle with plasma membrane. Ach release is prevented.
Use-eliminate frown lines & wrinkles, achalasia (abnormal esophageal contractions), strabismus, oromandibular dystonia (continuous spasm of face, jaw, neck). |
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Term
| Muscarinic Block on Heart |
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Definition
| Initial bradycardia due to block of inhibitory presynaptic M2 receptor, which transiently increases release of Ach. The tachycardia ensues from M2 block on SA node. |
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Term
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Definition
| Non selective agonist-alpha 1 & 2, Beta 1 Action: vasoconstriction, direct increase HR, reflexive decrease HR Use: hypotension Tox:hypertension, arrhythmias, headache |
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Term
|
Definition
Non-selective agonist-alpha1&2, Beta1&2 Action: increase HR, increase contractility, increase BP, reflexive decrease HR. Use: anaphylactic shock, with local anesthetics, glaucoma
tox: palpitation, arrhythmias, headache, tremor
Note: at high epi concentrations, alpha-1 receptors have dominant action. as conc declines beta-2 effects will take over, i.e. initial vasoconstriction followed by delayed vasodilation (incr MAP, decr MAP, HR via beta-1 will remiain elevated). |
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Term
|
Definition
Agonist-alpha1 selective agonist
Action: vasoconstriction
Use: nasal congestion (will cause decongestion with local vasoconstriction)
Tox: hypertension |
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Term
|
Definition
Alpha2 selective agonist (presynaptic auto-receptors & postsynaptic in CNS - decr peripheral sympathetic tone)
Action: decrease sympathetic outflow from CNS
Use: hypertension, used to tx withdrawal syndrome from opioids and alcohol.
Tox: sedation |
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Term
|
Definition
D1 selective agonist
Action: vasodilation (increase blood flow @ renal, mesenteric, CNS)
Use: hypertensive emergency, increase renal perfusion, anuria
Tox: postural hypotension |
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Term
|
Definition
Beta1 selective agonist
Action: increase contractility & HR
Use: cardiac decompensation (arrest), shock, heart block
Tox: tachyarrhythmias, hypertension |
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Term
|
Definition
Beta2 selective agonist
Action: relax bronchial & uterine smooth muscle
Use: bronchodilator for Asthma/COPD
Tox: tachycardia, muscle tremor |
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Term
|
Definition
Beta2 selective agonist
Action: relax bronchial & uterine smooth muscle (slow premature labor)
Use: bronchodilator for Asthma/COPD
Tox: tachycardia, muscle tremor |
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Term
|
Definition
Beta1&2 Non-selective Agonist
Action: decrease resistance, incr CO, incr HR, bronchodilation
Use: bronchodilator for asthma, shock, heart block
Tox: palpitation, tachyarrhythmias, headache |
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Term
|
Definition
Alpha1 selective antagonist
Action: vasodilation, decr resistance, decr BP
Use: primary hypertension, BPH
Tox: postural hypotension (usually first dose) |
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Term
|
Definition
Alpha1&2 antagonist
Action: vasodilation, decr resistance & BP
Use: pheochromocytoma, Raynaud's, frostbite
Tox: postural hypotension, inhibit ejaculation
Remember alpha 2 autoreceptors are present presynaptically. Blocking these leads to incr NE release which activates Beta1 & incr HR. |
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Term
|
Definition
Alpha1&2 antagonist
Action: vasodilation, decr resistance & BP
Use: pheochromocytoma, Raynaud's, frostbite
Tox: postural hypotension, inhibit ejaculation
Remember alpha 2 autoreceptors are present presynaptically. Blocking these leads to incr NE release which activates Beta1 & incr HR. |
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Term
|
Definition
Agonist: direct affect-D1 (low dose), Beta1 (medium dose), Alpha1 (high dose), NE release (indirect affect)
Action: vasodilation, incr GFR, HR, BP
Use: shock, renal failure, hypotension
Tox: vasoconstriction @ high doses |
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Term
|
Definition
Indirect acting release of NE
Action: CNS stimulation, incr BP & HR
Use: ADHD, narcolepsy, recreation
tox: hypertension, insomnia, anxiety, arrhythmias |
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Term
|
Definition
Indirect agent - agonist
Source: fermented foods (cheese & pickled herring)
Action: enters presynaps via uptake transporter & in exchange NE exits.
Use:
Tox: tachyphylaxis = acute tolerance - cytoplasmic pool of NE used up.
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Term
|
Definition
Neuron blocking drug - little clinical use, many serious side-effects.
management of pheochromocytoma |
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Term
|
Definition
Neuron blocking drug - little clinical use, many serious side-effects.
Action: interferes with vesicular transporter that picks up cytoplasmic DA, NE, HT, leading to empty vesicles. No NE is released.
Use: older hypertensive
Tox: suicide from serious depression |
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Term
|
Definition
Neuron blocking drug - little clinical use, many serious side-effects.
Action: has a unique affinity for vesicular transporter and instead of having NE, DA, HT repackaged, the vesicle is filled instead with Guanethidine.
Use: antihypertensive |
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Term
|
Definition
alpha agonist
Use: migraines |
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Term
|
Definition
alpha agonist
use: oxytocic-control post-partum bleeding (uterine contraction) |
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Term
|
Definition
DA & DA2 agonist
Use: hyperprolactinemia (decrease prolactin from pituitary via DA2 agonist), Parkinson via DA agonist. |
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Term
|
Definition
Alpha2 selective agonist (presynaptic auto-receptors & postsynaptic in CNS - decr peripheral sympathetic tone)
Action: decrease sympathetic outflow from CNS
Use: hypertension, used to tx withdrawal syndrome from opioids and alcohol.
Tox: sedation |
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Term
|
Definition
| Beta blocker, 1st generation, non-selective (Beta1&2) Action: decr HR & contractility & CO Use: angina, hypertension, arrhythmias Tox: bradycardia, bronchoconstricion, sexual dysfxn |
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Term
|
Definition
Beta blocker, 1st generation, non-selective (Beta1&2)
Action: decr HR & contractility & CO
Use: angina, hypertension, arrhythmias
Tox: bradycardia, bronchoconstricion, sexual dysfxn |
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Term
|
Definition
Beta blocker, 2nd generation, Beta1 selective antagonist
Action: decr HR & contractility & CO
Use: hypertension, angina, arrhythmias, CHF
tox: bradycardia, sexual dysfxn |
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Term
|
Definition
Beta blocker, 2nd generation, Beta1 selective antagonist
Action: decr HR & contractility & CO
Use: hypertension, angina, arrhythmias, CHF
tox: bradycardia, sexual dysfxn |
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Term
|
Definition
Beta Blocker, 3rd generation, non-selective Beta antagonist Action: decr HR & CO Use: CHF, hypertension
Additional Action: alpha-1 antagonist leading to vasodilation.
Tox: bradycardia, fatigue |
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Term
|
Definition
Beta Blocker, 3rd generation, non-selective Beta antagonist Action: decr HR & CO, decr TPR with little tachycardia
Use: CHF, hypertension
Additional Action: alpha-1 antagonist leading to vasodilation.
Tox: bradycardia, fatigue |
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Term
|
Definition
Beta Blocker, 3rd generation, Beta1 selective antagonist
Action: decr HR & CO
Use: CHF, hypertension
Tox: bradycardia |
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Term
|
Definition
NSAID
used to relieve symptoms in long-term tx of RA and other musculoskeletal disorders. |
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Term
|
Definition
NSAID
used to relieve symptoms in long-term tx of RA and other musculoskeletal disorders. |
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Term
|
Definition
COX-2 inhibitor
Use is superseding conventional NSAID as they decr the incidence of gastric & duodenal ulcers by 50% compared with traditional NSAIDs.
*these agents eliminate pain and some inflammation but DO NOT slow progression of disease. |
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Term
|
Definition
Glucocorticoid, suppress inflammation associated with RA.
Mech: inhibit PLA2, preventing release of arachidonic acid. Also inhibits production of cytokines, preventing induction of COX-2.
tox-hyperglycemia, osteoporosis, poor wound healing.
Can be used to induce a remission in disease at start of slower acting DMARD thx. |
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Term
|
Definition
Anti-malarial, tx RA that no longer responds to NSAIDs.
tox-causes retinal damage |
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Term
|
Definition
| Anti-malarial, tx RA that no longer responds to NSAIDs. tox-less side effects than chloroquine, which causes retinal damage |
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Term
|
Definition
acts quicker than anti-malarials.
inhibits IL-1 & TNF-alpha.
retards radiographic progression of RA
tox- N&V, headaches, skin rashes, leucopenia (cause about 30% of pts to discontinue drug). |
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Term
|
Definition
folate analog, most commonly used DMARD and considered gold std of DMARD thx.
mech-inhibit aminoimidazole carboxamide (AICAR) transformylase and thymydilate synthetase w/ secondary effects on polymorphonuclear chemotaxis.
Also inhibits rxn catalyzed by dihydrofolate reductase, essential for DNA sythesis, AICAR and TS inhibition is primary mechanism. |
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Term
|
Definition
pro-drug, taken orally
active metabolite inhibits dihydroorotate dehydrogenase (DHODH), rate limiting enzyme required for de novo synthesis of pyrimidine. It reduces both B & T cell populations, and generation of cytokines.
tox: diarrhea, hepatotoxicity |
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Term
|
Definition
fusion protein made up of 2 recombinant soluble TNF receptors fused with the Fc portion of human IgG1 (this fusion extents plasma half-life).
-twice weekly subQ injection result in significant improvement and are well tolerated. |
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Term
|
Definition
-chimeric mouse-human monoclonal IgG1 Ab against TNF-alpha.
-produces clinically significant improvement within a week of injection.
-murine monoclonal Ab are antigenic, and induce production of anti-mouse Ab. |
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Term
|
Definition
-fully human monoclonal anti-TNF-alpha Ab.
-as efficacious as etanercept, but with more convenient dosing regimen (2x monthly subQ). |
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Term
|
Definition
-soluble recombinant human IL-1 receptor antagonist.
-short (6 hour) half-life in plasma necessitates freq. daily tx with high doses. |
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Term
|
Definition
-inhibits T-cell activation
-induces T-cell apoptosis |
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Term
|
Definition
| -IL-6 receptor antagonist |
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Term
|
Definition
-anti-CD20 monoclonal Ab
-reduces circulating B-cells |
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Term
|
Definition
-for Acute Gouty Arthritis
-relieves pain & inflammation in 12-24 hours
-does not alter metabolism or excretion of urates
-binds tubulin and inhibits leukocyte migration, phagocytosis, metabolic activity, and release of proinflam autocoids.
tox- N&V, abdominal pain, and troublesome diarrhea due to inhibition of epithelial prolif.
-longterm use can cause neuropathy or blood dyscrasias (leukemia) |
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Term
|
Definition
-inhibit eicosanoid mediated pain & inflam.
-used for initial tx of acute gout or if colchicine unsuccessful or too much discomfort.
-commonly used NSAID (indomethacin, naproxen, sulindac, celecoxib). |
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Term
|
Definition
| -intraarticular injection good for acute monoarticular gout. |
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Term
|
Definition
Uricosuric Agent (increase rate of uric acid excretion), thx for chronic tophaceous gout.
-compete with urate at anionic transport site at renal tubule and inhibit reabsorption.
-tophaceous deposits of urate will be reabsorbed, with relief of arthritis and remineralization of bone.
tox-gastrointestinal irritation, reduced urate levels can cause urate mobilization and acute gouty arthritis. secretion of some week acids, notably penicillin, is reduced by these agents. |
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Term
|
Definition
-reduces uric acid synthesis by inhibiting xanthine oxidase, largely replacing uricosuric agents.
-allopurinol (competitive inhibitor) metabolized to alloxanthing (non-competetive inhibitor) by XO.
-for pts with high urnary uric acid and prevent massive uricosuria following chemo of leukemia, lymphomas and other malignancies that could otherwise lead to renal calculi.
tox-generally well tolerated, but like probenecid acute gouty arthritis may occur with mobilization of uric acid crystals. |
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Term
|
Definition
non-competetive inhibitor of xanthine oxidase.
tx chronic tophaceous gout |
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Term
|
Definition
Carbonic Anhydrase Inhibitor, proximal tubule
-induce moderate increase in urine volume with increased excretion of Na, K, HCO3 in an alkaline urine.
-induce a moderate reduction in ECF volume; hypokalemia and metabolic acidosis; ophtho to decr intraocular volume, acute mountain sickness.
-limited use as diuretic
tox-hypokalemia, metabolic acidosis, accumulation of ammonia in ECF (raise pH of tubular fluid prevents trapping of diffusing NH3 as NH4+ in tubule) which increases risk of hepatic encephalopathy and contraindicated in pts with cirrhosis.
Metabolic Acidosis causes kidney to become refractory to drugs and acidosis is corrected by reabsorbing more HCO3. |
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Term
|
Definition
Carbonic Anhydrase Inhibitor, proximal tubule
-induce moderate increase in urine volume with increased excretion of Na, K, HCO3 in an alkaline urine.
-induce a moderate reduction in ECF volume; hypokalemia and metabolic acidosis; ophtho to decr intraocular volume, acute mountain sickness.
-limited use as diuretic
tox-hypokalemia, metabolic acidosis, accumulation of ammonia in ECF (raise pH of tubular fluid prevents trapping of diffusing NH3 as NH4+ in tubule) which increases risk of hepatic encephalopathy and contraindicated in pts with cirrhosis.
Metabolic Acidosis causes kidney to become refractory to drugs and acidosis is corrected by reabsorbing more HCO3. |
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Term
|
Definition
Carbonic Anhydrase Inhibitor, proximal tubule
-induce moderate increase in urine volume with increased excretion of Na, K, HCO3 in an alkaline urine.
-induce a moderate reduction in ECF volume; hypokalemia and metabolic acidosis; ophtho to decr intraocular volume, acute mountain sickness.
-limited use as diuretic
tox-hypokalemia, metabolic acidosis, accumulation of ammonia in ECF (raise pH of tubular fluid prevents trapping of diffusing NH3 as NH4+ in tubule) which increases risk of hepatic encephalopathy and contraindicated in pts with cirrhosis.
Metabolic Acidosis causes kidney to become refractory to drugs and acidosis is corrected by reabsorbing more HCO3. |
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Term
| Aminophylline (theophylline) |
|
Definition
Proximal Tubule
Mechanism is unclear, but incr GFR. Also inhibits phosphodiesterase which incr cAMP which decr Na reabsorption in proximal tubule.
Modest incr in diuresis (5%). Mostly used to control inflammation and bronchospasm in asthma patients. |
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Term
|
Definition
Osmotic diuretics, proximal tubule
-increase rate and volume of urine due to filtration and presence of nonreabsorbable solute.
-increase osmolarity in prox tub fluid, opposing isotonic reabsorption of Na and H2O.
-similar to diabetes mellitus.
-mannitol is admin iv for incr clearance of drug, minimize renal failure during shock or surg, decr intraocular & intracranial pressure, dx of oliguria.
Also: excess glucose, urea, isorbide |
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Term
|
Definition
Loop/high ceiling diuretic, medullary and cortical talH, inhibits Na/K/2Cl co-transporter.
-most efficacious of diuretics, incr FE-Na up to 25%
-induces ECF volume contraction and a change in ECF solute concentration: hyperbicarbonatemia-alkalosis, hyperuricemia, incr BUN, incr creatinine (w/ decr GFR only).
-prompt onset of exceptionally large diuresis: crisis episodes of pulm edema & edema of CHF/cirrhosis, hypercalcemia, drug toxicity.
tox-hypokalemia-diabetes, hyponatremia, contraction alkalosis, hyperuricemia, incr BUN, incr creatinine, decr capacity of kidney to concentrate/dilute urine in response to decr/incr H2O consumption. Ototoxicity increased by aminoglycoside abx. |
|
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Term
|
Definition
Loop/high ceiling diuretic, medullary and cortical talH, inhibits Na/K/2Cl co-transporter.
-most efficacious of diuretics, incr FE-Na up to 25%
-induces ECF volume contraction and a change in ECF solute concentration: hyperbicarbonatemia-alkalosis, hyperuricemia, incr BUN, incr creatinine (w/ decr GFR only).
-prompt onset of exceptionally large diuresis: crisis episodes of pulm edema & edema of CHF/cirrhosis, hypercalcemia, drug toxicity.
tox-hypokalemia-diabetes, hyponatremia, contraction alkalosis, hyperuricemia, incr BUN, incr creatinine, decr capacity of kidney to concentrate/dilute urine in response to decr/incr H2O consumption. Ototoxicity increased by aminoglycoside abx. |
|
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Term
|
Definition
Loop/high ceiling diuretic, medullary and cortical talH, inhibits Na/K/2Cl co-transporter.
-most efficacious of diuretics, incr FE-Na up to 25%
-induces ECF volume contraction and a change in ECF solute concentration: hyperbicarbonatemia-alkalosis, hyperuricemia, incr BUN, incr creatinine (w/ decr GFR only).
-prompt onset of exceptionally large diuresis: crisis episodes of pulm edema & edema of CHF/cirrhosis, hypercalcemia, drug toxicity.
tox-hypokalemia-diabetes, hyponatremia, contraction alkalosis, hyperuricemia, incr BUN, incr creatinine, decr capacity of kidney to concentrate/dilute urine in response to decr/incr H2O consumption. Ototoxicity increased by aminoglycoside abx. |
|
|
Term
| Ethacrynic Acid (dichlorophenoxyaetic acid) |
|
Definition
Loop/high ceiling diuretic, medullary and cortical talH, inhibits Na/K/2Cl co-transporter.
-most efficacious of diuretics, incr FE-Na up to 25%
-induces ECF volume contraction and a change in ECF solute concentration: hyperbicarbonatemia-alkalosis, hyperuricemia, incr BUN, incr creatinine (w/ decr GFR only).
-prompt onset of exceptionally large diuresis: crisis episodes of pulm edema & edema of CHF/cirrhosis, hypercalcemia, drug toxicity.
tox-hypokalemia-diabetes, hyponatremia, contraction alkalosis, hyperuricemia, incr BUN, incr creatinine, decr capacity of kidney to concentrate/dilute urine in response to decr/incr H2O consumption. Ototoxicity increased by aminoglycoside abx. |
|
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Term
|
Definition
Thiazide diuretic, early distal tubule, inhibits Na/Cl co-transporter
-induce moderate diuresis, incr FE-Na 5-8%.
-induce ECF volume contraction and a change in ECF solute concentration: hyperbicarbonatemia-alkalosis, hyperuricemia, increased BUN & serum creatinine, hyponatremia/hypomagnesemia
use: control hypertension (major), chronic edema CHF, idiopathic hypercalciuria, nephrogenic diabetes insipidus-litihium thx.
tox: hypokalemia-diabetes, hyponatremia, contraction alkalosis, hyperuricemia, incr BUN & serum creatining, hypercalcemia, decr capacity of kidney to dilute urine and compensate for ECF volume expansion due to incr H2O consumption. |
|
|
Term
|
Definition
Thiazide diuretic, early distal tubule, inhibits Na/Cl co-transporter
-induce moderate diuresis, incr FE-Na 5-8%.
-induce ECF volume contraction and a change in ECF solute concentration: hyperbicarbonatemia-alkalosis, hyperuricemia, increased BUN & serum creatinine, hyponatremia/hypomagnesemia
use: control hypertension (major), chronic edema CHF, idiopathic hypercalciuria, nephrogenic diabetes insipidus-litihium thx.
tox: hypokalemia-diabetes, hyponatremia, contraction alkalosis, hyperuricemia, incr BUN & serum creatining, hypercalcemia, decr capacity of kidney to dilute urine and compensate for ECF volume expansion due to incr H2O consumption. |
|
|
Term
|
Definition
Thiazide diuretic, early distal tubule, inhibits Na/Cl co-transporter
-induce moderate diuresis, incr FE-Na 5-8%.
-induce ECF volume contraction and a change in ECF solute concentration: hyperbicarbonatemia-alkalosis, hyperuricemia, increased BUN & serum creatinine, hyponatremia/hypomagnesemia
use: control hypertension (major), chronic edema CHF, idiopathic hypercalciuria, nephrogenic diabetes insipidus-litihium thx.
tox: hypokalemia-diabetes, hyponatremia, contraction alkalosis, hyperuricemia, incr BUN & serum creatining, hypercalcemia, decr capacity of kidney to dilute urine and compensate for ECF volume expansion due to incr H2O consumption. |
|
|
Term
|
Definition
Thiazide diuretic, early distal tubule, inhibits Na/Cl co-transporter
-induce moderate diuresis, incr FE-Na 5-8%.
-induce ECF volume contraction and a change in ECF solute concentration: hyperbicarbonatemia-alkalosis, hyperuricemia, increased BUN & serum creatinine, hyponatremia/hypomagnesemia
use: control hypertension (major), chronic edema CHF, idiopathic hypercalciuria, nephrogenic diabetes insipidus-litihium thx.
tox: hypokalemia-diabetes, hyponatremia, contraction alkalosis, hyperuricemia, incr BUN & serum creatining, hypercalcemia, decr capacity of kidney to dilute urine and compensate for ECF volume expansion due to incr H2O consumption. |
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Term
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Definition
Thiazide diuretic, early distal tubule, inhibits Na/Cl co-transporter
-induce moderate diuresis, incr FE-Na 5-8%.
-induce ECF volume contraction and a change in ECF solute concentration: hyperbicarbonatemia-alkalosis, hyperuricemia, increased BUN & serum creatinine, hyponatremia/hypomagnesemia
use: control hypertension (major), chronic edema CHF, idiopathic hypercalciuria, nephrogenic diabetes insipidus-litihium thx.
tox: hypokalemia-diabetes, hyponatremia, contraction alkalosis, hyperuricemia, incr BUN & serum creatining, hypercalcemia, decr capacity of kidney to dilute urine and compensate for ECF volume expansion due to incr H2O consumption. |
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Term
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Definition
Thiazide diuretic, early distal tubule, inhibits Na/Cl co-transporter
-induce moderate diuresis, incr FE-Na 5-8%.
-induce ECF volume contraction and a change in ECF solute concentration: hyperbicarbonatemia-alkalosis, hyperuricemia, increased BUN & serum creatinine, hyponatremia/hypomagnesemia
use: control hypertension (major), chronic edema CHF, idiopathic hypercalciuria, nephrogenic diabetes insipidus-litihium thx.
tox: hypokalemia-diabetes, hyponatremia, contraction alkalosis, hyperuricemia, incr BUN & serum creatining, hypercalcemia, decr capacity of kidney to dilute urine and compensate for ECF volume expansion due to incr H2O consumption. |
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Term
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Definition
Renal epithelial sodium channel inhibitor, late distal tubule and collecting duct, block luminal Na channels and Na/H exchanger.
-K sparing diuretic, aldosterone independent, weak base
-induces moderate diuresis, incr FE-Na 2%, used in combination with thiazide or loop diuretics to minimize K depletion.
use: combo to spare K, edema CHF/cirrhosis/nephrotic syndrome, idiopathic hypercalciuria, Li induced polyuria.
tox: hyperkalemia
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Term
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Definition
Renal epithelial sodium channel inhibitor, late distal tubule and collecting duct, block luminal Na channels and Na/H exchanger.
-K sparing diuretic, aldosterone independent, weak base
-induces moderate diuresis, incr FE-Na 2%, used in combination with thiazide or loop diuretics to minimize K depletion.
use: combo to spare K, edema CHF/cirrhosis/nephrotic syndrome, idiopathic hypercalciuria, Li induced polyuria.
tox: hyperkalemia
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Term
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Definition
Aldosterone receptor antagonist, late distal tubule and collecting duct, binds AR competitively and reduces mRNA for Na absorption and K secretion, indirect inhibition of Na/H exchanger.
-K sparing diuretic, aldosterone dependent
-induces moderate diuresis, incr FE-Na 2%, used in combination with thiazide or loop diuretics to minimize K depletion.
use: combo to spare K, edema CHF/cirrhosis/nephrotic syndrome, primary/secondary aldosteronism, idiopathic hypercalciuria, Li induced polyuria.
tox: hyperkalemia, gender-specific, effects of androgen receptor antagonism by spironolactone.
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Term
| Determinants of Diuretic Activity |
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Definition
Activity is dependent on drug conc. at site of action in nephron.
-plasma conc, renal blood flow, GFR, tubular secretion (organic anion & organic cation transporters), tubular fluid conc.
Use of diuretics in pts with renal disease
-renal failure, nephrotic syndrome |
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