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5 major classes of diuretics
- Osmotic
- Carbonic anhydrase inhibitors
- thiazides
- organic acid/loop
- Potassium sparing
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Osmotic diuretics
- filtered by glomerulus but not reabsorbed so it is excreted
- create osmotic gradient, water migrates and follows the molecule
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Osmotic diuretic drug
Mannitol
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Mannitol
- osmotic diuretic
- can't penetrate membrane so it must be taken by IV
- used in acute renal failure
- useful in drug overdoses; used to help water to follow to excrete drug used in overdose
- increases systemic blood volume
- shouldn't be given to those who have compromised cardiac function
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Carbonic anhydrase inhibitors
- increase Na+ and H2O by inhibiting carbonic anhydrase
- enzyme produces H+ and biocarbonate (HCO3) from CO2 and H2O; so CA inhibitors block the reaction above so we are left wtih CO2 and H2O
- takes place in proximal and distal tubules
- MAJOR SIDE EFFECT: alter acid/base balance
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Carbonic anhydrase inhibitors drug
Acetazolamide
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Acetazolamide
- carbonic anhydrase inhibitor
- used for glaucoma
- mainly used for toxicity
- body attempts to exchange potassium wtih Na, so lose potassium
- major problem is it alters acid/base balance
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Thiazide diuretics
- inhibit Na+ reabsorption
- increase Cl- and K+ excretion as well
- orthostatic hypotension
- MAJOR SIDE EFFECT: loss of K+
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Thiazide drug
Hydrochlorothiazide
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Organic Acid/loop
- inhibits Na+/Cl- transport in loop of henle
- common side effect: tone deafness which is reversible, when off the drug hearing will come back
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Organic Acid/loop
Lasix (furosemide)
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Potassium Sparing diuretics
- used in conjunction with loop and thiazides to compensate for loss of K+
- inhibits K+ excretion
- Spirolactone -> antgonist of aldosterone receptors which excretes K+ secretion
- MAJOR SIDE EFFECT: prolongs repolarization and collides with cardiac glycosides
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Potassium sparing diuretics drug
Amiloride
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Amiloride
- Potassium sparing diuretics drug
- alters membrane so K+ can't be secreted
- major side effect: prolongs repolarization and collides with cardiac glycosides
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Anti-psychotic drugs
- work through serotonin and dopamine receptors
- Phenothiazines
- Butyrophenones
- Thioxanthenes
- Atypical anti-psychotics
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Phenothiazines
- three main side effects:
- 1)dystonic reactions (muscle spasm)
- 2)Akathisia (continous body movement)
- 3)Parkinsonism
- Block D2 receptor, histamine receptors, AcH receptor, and alpha adrenergic
- interacts with serotonin to cause weight gain and therapeutic effect
- no control over secretion
- blurred vision, constipation, dry mouth and eyes, hypotension, drooling on yoruself
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Butyrophenones
- D2 antagonists
- minimal mACH
- fewer side effects than phenothiazines but they produce strong movement distributions
- interact with alpha adrenergic but not histamine (sedation)
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Butyrophenone drugs
- Haldol (one of first drugs for people with turrets)
- Haloperidol (more potent and produces fewer side effects; main effects on dopamine)
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Atypical anti-psychotics
- D2 receptor antagonist
- Serotonin blockade (blocks serotonin)
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Atypical anti-psychotic drugs
- Aripiprazole (Abilify)
- Resperidone - same receptors as abilify but different structures
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Benzodiazepines
- work by GABAa receptors (they do not bind directly onto receptors)
- respiratory, Cardiovascular, and CNS depression
- benzodiazepine receptors are co-localized on GAABA receptors
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Pentylentetrazol
GABA antagonist
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Mania
- hyperexcitability and elation
- appears to be excess of Norepi
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Treatment for mania
- lithium
- body uses lithium for sodium and disrupts neuronal action
- increase uptake of dopamine and norepi
- dopamine is then retaken up and broken down by monoamine oxidase (MAO) so less will interact with receptors to create excitability
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Anti-depressant classes
- Monoamine oxidase inhibitors
- Tricyclic anti-depressants
- Selective serotonin reuptake inhibitors (SSRI)
- Atypical anti-depressants
- Herbal supplements
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Monoamine oxidase inhibitors
- oldest class of anti-depressants and still widely used
- very cheap (30 day prescription fr 1.50)
- inhibits MAO and there a buildup of NE and 5-HT in synaptic cleft
- dietary restrictions: no wine, cheese, or beer since they have tyarmine
- insomia, convulsions, tremors
- really potent and many side effects but usually last choice unless financial situations
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Monoamine oxidase inhibitor drug
Phenylzine
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Tricyclic anti-depressants
- block reuptake of norepi and serotonin in nerve endings
- causes sedation, tremors or mania by blocking alpha adrenergic and cholinergic receptors
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Tricyclic anti-depressant drugs
Nortriptyline (aventyl)
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Selective serotonin reuptake inhibitors (SSRI)
- little to no action on cholinergic and adrenergic recptors
- block reuptake of serotonin
- serotonin syndrome: too much serotonin in synaptic cleft which increases cardiovascular activity and causes tremors
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SSRI drugs
- Sertraline (zoloft)
- Fluoxetine (prozac)
- Paxil - used to treat children under 10 for depression and increased suicidal tendencies
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Atypical anti-depressants
- block serotonin and norepi or dopamine
- little to no cholinergic or adrenergic activity
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Atypical anti-depressant drugs
- Bupropion (wellbutrin) - inhibit dopamine and norepi reuptake; sometimes prescribed to weight loss but you can become psychotic
- Venlafaxine (effexor) - inhibit serotonin and norepi reuptake
- Duloxetine (cymbalta) - inhibit serotonin and norepi reuptake
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Herbal supplements
- St. John's wort:
- serotonin and norepi reuptake inhibitors
- drug interactions
- not FDA regulated b/c the label does not say to treat depression but instead mood
- Valarian:
- anti-anxiety
- binds to dopamine receptor
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Drugs used for Epilepsy
- Barbituates
- K+/Na+ bromide
- Carbamazepine (drug)
- Gabapentin (drug)
- Keppra (leutiracetam)
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Barbituates
- developed in 1912
- phenobarbitol
- binds directly to GABA receptor and acts as agonist to produce sedative effects
- side effects: puts to sleep, lipid soluble and addicive
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Carbamazepine
- blocks Na+ channels
- decrease action potential
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Gabapentin
- interacts with Ca++ chanels
- decrease conduction across syapses
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Keppra (leutiraetam)
- inhibits Ca++ channels
- decreases conduction across synapses
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Illicit drugs
- Amphetamines
- Cocaine
- LSD
- Bath Salts
- Spice or K2
- 2-CI or smiles
- Phenylcycldine (PCP)
- Ketamine
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Amphetamines
- treatment of ADHD, weight loss, narcolepsy, and hypotension
- inhibits reuptake of serotonin, norepi, and dopamine
- increase release of neurotransmitters
- decrease fatigue
- increase aggresion
- decrease human empathy
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Amphetamine drugs
- Adderall (amphetamine and dextroamphetamine)
- Ritalin (methylphenalate)
- Stratthera (amoxetine)
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Cocaine
- blocks reuptake of NE and dopamine
- increases sympathetic activity, euphoria, stimulation of motor system
- first person to use was Freud on his family
- blocks Na+ channels
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What drug is used to reverse effects of cocaine?
benzos (benzodiazepam) used for overdose
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LSD
- serotonin agonist
- hallucinations
- no known death associated with LSD
- synthesia (see sounds)
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Bath Salts
- MDPV (methylenedioxypyrovalerone)
- bath salts don't have a half life like cocaine which will lessen effects as it leaves body)
- 100x more potent than cocaine
- target 5-HT, NE, dopamine
- increase blood pressure, heart rate, aggitation, and delusions
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Spice or K2
- synthetic cannabinoid
- 4-5x more potent than THC and won't show up in drug test
- JWH-018
- JWH-073
- jwh stands for company
- and # stands for derivative
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2-CI or Smileeffect
- class of drugs similar to phenythethyamine (produced in body; NE and dopamine)
- simliar to amphetamine
- hallucinations
- increase sympathetic activity
- taken orally no effect b/c of first pass effect
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Phencyclidine (PCP)
- Ketamine (derivative of PCP; used in animales)
- blocks glutamate activated NMDA receptors
- originally produced as anaesthetic
- disorientation,mania, hallucinations
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Opiod Analgesics
- block bain receptors; used for dental, trauma, cancer, post-operative, visceral
- Dextromethorphan (weak opiod over the counter)
- Morphine (first opiod)
- Heroin was produced (ended up being 3-4x more potent;heroin ends up being metabolized to morphien and binds to mu,kappa form receptors to produce therapetuic properties)
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Methadone
- very weak opiod agonist
- 1/2 potent as morphine
- used to ween you off of morphine or heroin
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Noloxone
- antagonist opiod
- blocks receptors and effects
- used in overdose
- mu receptor antagonist
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Suboxone
- combo of naloxone and buprenorphine
- more potent than noloxone itself
- used in overdose
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Codeine and dextromethorphan
anti-tussive (suppress cough reflex) opiod
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most common side effect of opiod?
nausea and vomiting
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Acute Coronary syndrome
- nitrates - nitroglycerin
- verapamil (ca++ channel blocker)
- prazosin (alpha 1 blocker)
- diazepam or barbitols increase sedation and decrease sympathetic activity
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Hypertension
diazepam or prazosin
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Edema
- diuretic
- lasix (loop diuretic)
- decrease sodium absorption so it can be eliminated
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Parkinson's
- loss of dopamine crucial for disease progression
- chief symptoms: tremors at rest, muscle rigidity, suppression of voluntary movements
- causes are viral infections, brain tumors, and other diseases
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Treatments for Parkinson's
- L-dopa:
- precursor to dopamine (easily corsses blood brain barrier to easily go to dopa receptors)
- increases dopamine synthesis
- usually given with carbidopa which inhibits the production of L-dopa decarboxylate)
- Dopamine receptor agonist:
- useed in combination with L-dopa for severe parkinsons
- specific drug = bromocriptine
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Bromocriptine
Dopamine agonist used for parkison's in later stages
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Alzhemier's
- loss of cholinergic synapses -> AcH signalling
- AcHesterase inhibitors which increases AcH in synapse to interact wtih receptor
- NMDA-glutamate: too much glutamate causes excitatoxicity
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drug used for Alzhemiers
- Aricept (donepezil) used therapeutically
- NMDA Antagonists such as Namenda (momantine) used for dementia associated with Alzheimers
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