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Cell Path > Drugs to Know > Flashcards

Drugs to Know Flashcards

1
Q

Acetominophen

A
  • Normally GSTs catalyze reaction of transferring GSH (glutathione) to NAPQI -> inactive form that gets eliminated
  • If OD –> deplete glutathione and accumulate NAPQI which kills liver and kidney cells (TOXIC)
  • Tylenol
  • Fever and pain reducer
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2
Q

Acetylcholine

A
  • Nicotinic and muscarinic receptors
  • Can be used to reduce pupil size in eye (inc miosis in ocular surgery); give intra-ocularly NOT systemically
  • LOCAL EFFECTS
  • Can give local infusion - will work on muscarinic receptors on vessels –> local vasodilation to inc blood flow tot hat area w/o systemic dec in BP
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3
Q

Albuterol

A

Beta 2 agonist

-bronchodilator (for asthma)

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4
Q

Alpha Methyl Dopa

A

central alpha 2 agonist –> dec central symp outflow (vasomotor center) bu inc inhibitory effect of these alpha 2 receptors–> dec BP

safe in pregnancy; so anti-hypertensive for pregnant women

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5
Q

Alpha Methyl Tyrosine

A

Sympatholytic

Inhibits tyrosin hydroxylase - dec in catecholamine synthesis

Synthetic tyrosine analogue

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6
Q

Amphetamine

A
  • Leads to inc NE release –> extracellular fluid
  • How? by inc exocytosis and inc release of NE from vesicle
  • Crosses BBB so CNS effects
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7
Q

Atracurium

A
  • Neuromuscular blocking agent
  • Non-depolarizing, competitive
  • Intermediate duration

In general…- Bind at same site at acetylcholine - only need to bind one of two alpha sites

- Dec frequency of channel opening
- Progression: motor weakness —> small rapidly moving muscles like eyes and jaw go first —> limbs/trunk —> intercostals —> diaphragm
    - **Regained in reverse order
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8
Q

Atropine

A

Muscarinic antagonist (no effect on nicotinic receptors)

  • Inhibit cholinesterase inhibitor toxicity (nerve gas exposure)
  • good at .5-1 mg then bad CNS effects (because it crosses the BBB)
  • at low dose it slows heart by M2 inhibitory receptors
  • balance cardio effects of neostigmine in surgery, dilate eye, reduce bronchial contraction and secretion in lungs,
  • side effects= dry mouth urinary retention
  • Crosses BBB so also causes sleepiness
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9
Q

Carbachol

A
  • MIOSTAT

- Used to close eye for protection in surgery (but slower onset and longer duration than local acetylcholine infusion)

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10
Q

Clonidine

A

Central alpha 2 agonist

Treats hypertension by dec symp tone (from vasomotor center)

Dec both cardiac output and TPR

Useful in hypertensive emergency- quick effect

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11
Q

Cocaine

A
  • Blocks dopamnie and serotonin receptors for termination (blocks SERT, DAT and NET)
  • Dec transport of NE back into cell –> more NE at receptors
  • Overdose can lead to adrenergic crisis
  • Crosses BBB so CNS effects
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12
Q

Diazepam

A

VALIUM

  • benzo
  • Inc GABA affinity for GABA A receptor –> inc Cl- into cell (so need GABA present to work); inc frequency of opening NOT duration of opening
  • Anti-anxiety, treats seizures, treats alcohol withdrawal and insomnia
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13
Q

Dopamine

A
  • Catecholamine
  • DA > B1&raquo_space; a1
  • @ low dose DI induced inc in blood flow (vasodilation)- including inc blood flow to kidneys
  • @ medium dose…beta 1 -induced in contractility w/o effect on BP
  • @ high dose …alpha 1 -induced inc in BP (used for SHOCK)

-Also mixed acting (both inc release of catecholamines and works right on receptors)

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14
Q

Edrophonium

A
  • Used to diagnose m. gravis (because short onset and short duration)
  • If temporary relief of symptoms then pos diagnosis
  • Cholinesterase inhibitor
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15
Q

Ephedrine

A

Non-selective adrenergic agonist (alpha and beta)

Mixed acting (so can inc NE release or act right on adrenergic receptor)

Inc BP, decongestant and bronchodilator

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16
Q

Epinephrine

A
  • @ low dose … beta 2 agonist … inc contraction and heart rate while dec in peripheral resistance (beta 2 vasodilation)
  • @ high dose… alpha agonist …inc vascular resistance and thus inc BP; also dec renal blood flow while inc muscle blood flow (beta 2 vasodilation is now offset by alpha vasoconstriction)
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17
Q

Flumazenil

A
  • Used for benzo overdose
  • GABA A receptor antagonist; binds to same spot on receptor as benzos; short half-life (30-60 min) so must monitor closely
  • If too much can lea to withdrawal seizures
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18
Q

Ganacurium

A

Non-depolarizing neuromuscular block

In general…- Bind at same site at acetylcholine - only need to bind one of two alpha sites

- Dec frequency of channel opening
- Progression: motor weakness —> small rapidly moving muscles like eyes and jaw go first —> limbs/trunk —> intercostals —> diaphragm
    - **Regained in reverse order

May replace succinylcholine b/c also ultra-short onset and duration but is non-depolarizing

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19
Q

Glycopyrrolate

A

Muscarinic Antagonist

Used to block sinus or nodal bradycardia (reverse effects of neostigmine) AKA inc HR

Does not cross BBB (unlike atropine) so does not cause sleepiness and other CNS effects

Also decreased secretions

Charged molecule

20
Q

Guanethidine

A
  • Sympatholytic
  • Replace NE n vesicles/prevent NE release from storage vesicles
  • Antihypertensive
  • Uses Uptake 1 to get into pre-synaptic terminal where it can then act on NE neurotransmission
21
Q

Ipratropium

A

ATROVENT

Used to treat COPD

Muscarinic antagonist

Charged

Does not cross BBB

22
Q

Isoproterenol

A

beta agonist (B1»B2)

-inc HR w/o changing BP; bronchodilator; inc cardiac output (BUT HIGH O2 DEMAND)

Ionotropic and vasodilator (works on beta 2 on vessels)

23
Q

Lidocaine

A

amine LA (long lasting; more stable)

  • Stabilize inactive form of ion channels…inability to produce action potential
    • DO NOT BLOCK CHANNEL ITSELF
    • Bind to the wall of the channel pore —> conformational change

Aniline or benzoic acid linked to tertiary amine via amide bond

24
Q

Methacholine

A

Direct muscarinic agonist

  • Used to diagnose airway hypersensitivity (people w/ asthma will have response w/ lower dose of drug than normal person)
  • Non-selective
25
Q

Modanifil

A

PROVIGIL “wake promoting agent”

  • psychostim (inc sleep vigilance and dec need for sleep)
  • For narcolepsy, sleep disorder due to shift work or sleep apnea)

Amphetamine-like sympathomimetic

Central alpha1 agonist??

26
Q

Muscarine

A

acts on muscarinic receptors –> parasymp response

Toxic- mushroom poisoning

27
Q

Neostigmine

A

Cholinesterase Inhibitor

  • Reversible
  • Treat m. gravis (because longer lasting than edrophonium but does not cross BBB so no CNS effects )
  • In surgery… reverse paralysis from neuromuscular block (given w/ glycopyrrolate so no anti-muscarinic effects) and reverse anti-muscarinic effects of inc HR
28
Q

Nicotine

A

acts on nicotinic receptors at ganglia and NMJ

addictive b/c desensitization

when it works on ganglia- enhances underlying tone (symp or parasymp) - tachycardia, inc BP, sweating

29
Q

Norepinephrine

A
  • catecholamine
  • Mainly alpha effects (works on beta to inc HR but only transient b/c body compensates for now high BP from alpha effects –> slows HR back down via baroreceptors)
  • Inc peripheral resistance/ inc BP
  • dec renal, cutaneous and muscle blood flow (unlike dopamine - which inc renal blood flow)
30
Q

Organophosphates

A

Cholinesterase Inhibitor

  • Irreversible (ages the enzyme)
  • Insecticides, nerve gas (serin, VG, VX), DFP (drug)
31
Q

2-PAM

A

Treat cholinesterase inhibitor toxicity (esp in military)

Must use right away b/c only works b/f the receptor has aged

32
Q

Pancuronium

A

Non-depolarizing neuromuscular block

Competitive inhibitor

Long duration

In general…- Bind at same site at acetylcholine - only need to bind one of two alpha sites

- Dec frequency of channel opening
- Progression: motor weakness —> small rapidly moving muscles like eyes and jaw go first —> limbs/trunk —> intercostals —> diaphragm
    - **Regained in reverse order
33
Q

Phenobarbital

A

LUMINAL

  • barbiturate
  • Directly activates GABA A receptor to keep Cl- channel open longer (but considered reversible)
  • anti-seizure and sedative/hypnotic effects
  • induces certain CYPs –> potential drug interactions
34
Q

Phenylephrine

A
  • Alpha 1 agonist (JUST ALPHA)

- Ocular/nasal vasoconstrictor (decongestant), acute vasopressor

35
Q

Physostigmine

A

Cholinesterase Inhibitor

  • Reversible
  • Not used to treat m gravis b/c crosses BBB (CNS effects)
  • Can cause seizures
  • Can also reverse effects of atropine OD in CNS since both cross the BBB
36
Q

Propanolol

A

non-slective beta agonist (BETA BLOCKER)

  • INDERAL
  • Can cause dec in exercise capacity b/c blocks the beta 2 receptors on vessels going to muscle - no vasodilation to inc blood flow to muscles when exercising
37
Q

Prozosin

A

MINIPRESS

selective alpha 1 antagonist (blocks receptors directly)

antihypertensive b/c prevents alpha 1 vasoconstriction

38
Q

Pyridostigmine

A

Cholinesterase Inhibitor

  • Reversible
  • Treat m. gravis b/c does not pass BBB
39
Q

Reserpine

A

inhibit transport of NE into storage vesicles –> deplete vesicular NE –> subsequent destruction by MAO inside pre-synaptic cell

So overall has a sympatholytic effect

Blocks VMAT (enzymes that loads NE into vesicles for release into synapse)

40
Q

Scopolamine

A

Muscarinic antagonist

Used to treat motion sickness (usually patch)

Dec vestibular muscarinic effects

Central- crosses BBB to have effects on CNS

Also causes euphoria —> abuse (“mad as a hatter”)

41
Q

Succinylcholine

A

Depolarizing neuromuscular block

quick b/c degraded by cholinesterase (unless using cholinesterase inhibitor)

Short onset and ultra-short duration so used for quick procedure such as intubation

Eliminated by butylcholinesterase NOT acetylcholinesterase

If prolonged apnea after use - patient may have dec levels of plasma butyl cholinesterase

42
Q

Tamsulosin

A

alpha 1 selective antagonist

Treat benign prostate hypertrophy

Blocks alpha 1 receptors in bladder smooth muscle and in prostate to enhance urine flow (b/c prostate hypertrophy inhibits urine flow)

43
Q

Terbutaline

A

beta 2 agonist

delay labor (dec contractions in premature labor) and short-acting bronchodilator

44
Q

Tolterodine

A

Muscarinic antagonist w/ partial receptor selectivity

Competitive antagonist - synthetic derivative to competes w/ acetylcholine at receptor site

For neuronal/urge urinary incontinence (not stress incontinence)

45
Q

Tropicamide

A

Synthetic muscarinic antagonist

Short duration - short acting paralysis of eye muscles

Used by eye Dr for dilation of eye for procedures

Lose ability to see near-sight

46
Q

Tyramine

A
  • Indirect acting sympathomimetic
  • Promote NE exocytosis or NE displacement from vesicles–> accumulation of NE at receptor sites (similar to amphetamines)
  • In diet (aged cheese, poultry, fish, wine, beer, yeast, beans) but normally degraded by MAO in liver - so usually only a problem if taking MAO inhibitors (class of anti-depressants)

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