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Drugs Block 1 Flashcards

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1
Q

Acetylcholine site of action, effect on the body (PD), body’s effect on the drug (PK), Therapeutic uses?

A

Site of Action: Muscarinic and Nicotinic
PD: DUMBBELS - Dirty drug
PK: AchE hydrolyzes in 5-30 seconds
Tx: cataract & ocular surgies (miosis)

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2
Q

Bethanechol site of action, effect on the body (PD), body’s effect on the drug (PK), Therapeutic uses?

A

Site of action: Muscarinic
Big Beth doesn’t like Che’s Pancreas
PD: Bowels, Bladder, 30 min - 2 hr
PK: ChE has no effect on her, orally active
Tx: ileus, urinary retention, test for pancreatic enzyme function.

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3
Q

Carbachol/Carbamylcholine site of action, effect on the body (PD), body’s effect on the drug (PK), Therapeutic uses?

A 
Carbon Copy of Acetycholine
Carbachol is smoll (small) -- eyes only 
PD: DUMBBELS - Dirty Drug
PK: 30 min - 2 hr
Tx: miosis in ocular surgery, chronic control of Open angle glaucoma
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4
Q

Pilocarpine site of action, effect on the body (PD), body’s effect on the drug (PK), Therapeutic uses?

A

“Cry, drool and sweat on your pilo”
Site of Action: Muscarinic, tertiary so basal ganglia too
PD: tears, saliva, sweat
PK: 30 min- 2 hr, AChE don’t work
Tx: xerostomia from Sjorgen’s/radiation therapy

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5
Q

What are the direct acting Cholinomimetics? Which ones can cross the BBB?

A

Acetylcholine, bethanechol, carbachol, and pilocarpine. Pilocarpine can affect CNS.

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6
Q

What are indirect acting cholinomimetics?

A

These drugs inhibit AChE

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7
Q

What is cholinesterase aging?

A

Aging occur when a drug binds to the anionic site on AChE. The drug will leave but the quarternary amine will stay, like a tick head when you only pull off the body! Only occurs with irreversible insecticides.

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8
Q

What are the reversible indirect acting cholinomimetics? Which ones cross the BBB? Where do these act?

A

Physostigmine, neostigmine, Pyridostigmine, Edrophonium. Physostigmine can cross the BBB. All indirects act on where AChE is (both muscarinic and nicotinic)

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9
Q

Physostigmine site of action, effect on the body (PD), body’s effect on the drug (PK), Therapeutic uses?

A

Site of action: M&N
PD: Tertiary, gets in CNS fast, lipid soluble, orally active, DUMBBELS
Body’s effect on drug: 30 min - 2 hr,
Tx: PHYxes atropine overdose (cholinolytic mushrooms), dirty so glaucoma surgery

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10
Q

Neostigmine site of action, effect on the body (PD), body’s effect on the drug (PK), Therapeutic uses?

A

Site of action: M&N, NMJ
PD: inhibits AChE
PK: slowly hydrolyzed by pseudocholinesterase and AChE, up to more than 2 hrs
Tx: like Big Beth: Bladder, Bowels, NeostiGMine (Gravis Myasthenia)

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11
Q

Pyridostigmine site of action, effect on the body (PD), body’s effect on the drug (PK), Therapeutic uses?

A

Site of Action: M&N, NMJ
PD: long duration, doesn’t penetrate CNS
PK: 4-8 hours
Tx: PyridosiGMine (Gravis Myasthenia)

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12
Q

Edrophonium site of action, effect on the body (PD), body’s effect on the drug (PK), Therapeutic uses?

A

Site of Action: M&N
Short! Only a DROP of eDROPhonium by IV
Tests to see if crisis is from Myasthenia Gravis or Cholinergic. If MG, things improve. If cholinergic, things DROP!

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13
Q

Carbamate Insecticides

A

AchE inhibitors, tx with atropine

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14
Q

What What are the irreversible indirect acting cholinomimetics?

A

There are the Organophosphate Insecticides that irreversibly inhibit AChE. These are very dangerous since it takes a couple days to regenerate AChE endogenously. Diisopropylflurophosphoroate, Echothiophate

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15
Q

How do you treat Overdose or accidental poisoning by Organophosphates?

A
  1. support vital signs
  2. decontaminate
  3. Atropine to block excessive muscarinic excitation
  4. Give 2-Pralidoxime to rejuvinate AChE, which is a competitive inhibitor to Organophosphates
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16
Q

What is Diisopropylfluorophsphorate?

A

orangophosphate insecticide which Irreversible binds AChE. Affects all cholinergic synapses and CNS. Long acting, used as a topical treatment for glaucoma.

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17
Q

What is Echothiophate?

A

Organophosphate, quatenary amine, poor oral absorption, long acting miotic for open angle glaucoma.

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18
Q

Metoclopramide site of action, effect on the body (PD), and therapeutic uses

A

Site of action: Dopamine receptor ANtagonist
PD: Increases GI motility and Gastro-esophageal pressure. No effect on HCl secretions.
Tx: with opiates like morphine to prevent constipation, before colonoscopy, hasten barium contrast. SE: drowsiness, lots of pooping

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19
Q

What are the three phosphidiesterase inhibitiors and what do they do?

A

Sildenafil, Tadalafil, Vardenafil. Fil the penis.
Sildenfil & Vardenafil: drug interactions with CYP450-3A4.
Tadalafil has duration of 36 hours. “Tada, thats a long acting drug”
Don’t use any of these drugs with nitrates. Find different angina drug.

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20
Q

What is the function of the cholinolytics?

A

Prevent agonist (ACh) binding, bind M3 receptors

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21
Q

What are the uses of Atropine?

A

Ocular uses primarily for mydriasis, found in deadly nightshade and jimson weed

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22
Q

What is tropicamide?

A

Cholinolytic, mydriatic

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23
Q

What is oxybutyniun?

A

cholinolytic, used to treat incontinence and urgency

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24
Q

What are adverse effects of cholinolytics?

A

xerostomia, cycloplegia, photophobia, CNS stimulation/depression, acute glaucoma due to closed iris/cornea angle, tachycardia, anhydrosis, heat stroke, urinary retention

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25
What is Ipratropium?
Used as a bronchodilator in treatment of COPD. Cholinolytic.
26
What is the effect of a ganglionic blockade in arterioles and veins?
vasodilation, increases peripheral blood flow in arterioles; venous pooling of blood and decreased cardiac output. Sympathetic activity blocked
27
What is the effect of a ganglionic blockage in the heart, iris, ciliary body, GI tract?
Heart - tachycardia Iris - mydriasis Ciliary - cycloplegia (muscle paralysis & loss of accomodation) GI Tract - decreased motility, constipation
28
What is the effect of a ganglionic blockade in bladder, salivary glands, and sweat glands
bladder - urinary retention salivary glands - xerostomia Sweat glands - anhidrosis
29
What are therapeutic uses for ganglionic blockers. Why limited use?
Limited use- dirty drugs, act on everything! Tx: hypertensive cardiovascular disease emergency, controlled hypotension in surgery (skin dissection or neurosurgery to produce blood less field), autonomic hyperreflexia (spinal cord injury), acute pulmonary edema (reduce pulmonary vascular resistance)
30
What are nicotinic receptor agonists?
nicotine. at low doses stimulates everything. At high doses, goes from being receptor agonist to antagonist "depolarizing inhibition"
31
What are 3 examples of nicotinic-ganglionic receptor blockers?
Hexamethonium (not clincally used) Mecamylamine (can enter CNS) Trimethaphan
32
What are adverse effects of ganglionic blockers?
visual disturbances, xerostomia, urinary retention, impotence, CNS stimulation followed by depression, marked hypotension, orthostatic hypotension, constipation
33
What is Tubocurarine?
a drug that has poor oral absorption, but long lasting because excreted by liver and kidney. Competitive nicotinic blocker (Nm antagonist), weak ganglionic blockade. Decreased BP, Venous Return, Vasodilation. Release of histamine causes vasodilation and bronchoconstriciton.
34
What are therapeutic uses of NM blockers
muscle relaxation during surgery/anesthesia, prevent elctroconvulsive therapy trauma, and reduce muscle spasms
35
What is Vecuronium?
Competitive NM blocker (antagonist), short acting). No histamine release so no changes in BP or HR.
36
What is Mivacurium?
Competitive NM blocked (antagonist), ultrashort onset and duration of action (10min). Hydrolyzed by plasma cholinesterases. No effect on ganglionic transmission or cardiac M2 receptors.
37
Succinylcholine?
NM agonist that works by depolarizing inhibition. Dirty drug but works fast so widely used. Fast onset, short acting (few minutes), releases Histamine, hydrolyzed by pseudocholinesterase.
38
Side effects of succinylcholine
release of K+ can result in arrthymias (gate left open), Decreased HR, BP (vagal response) or increased BP (sympathetic). 1/2500 have abnormal cholinesterase so prolongued effect. Tx: serum cholinesterase P behring
39
What are adverse effects of Neuromuscular blockers?
Histamine relaxes arterioles, Ganglionic blockade, pooling blood in muscles with paralysis
40
Antidote for nondepolarizing blockers?
Mivacarium, Vecuronium, and tubocurarine - Give neostigmine or other AChE inhibitor and support respiration.
41
What does dantrolene do?
blocks release of calcium, used to treat spasticity due to stroke and other neuro conditions. No calcium = no contraction.
42
What are side effects of dantrolene?
muscle weakness, fatigue, diarrhea, liver dysfunction (CI - liver disease & respiratory muscle weakness)
43
Treatment for succinyl choline?
Tx: serum cholinesterase P behring (only if AChE is low)
44
What is a treatment for malignant hyperthermia (also how is it caused)?
Dantrolene. Caused when combine gaseous anesthetics and succinylcholine.
45
What is malignant hyperthermia syndrome?
NM rigidity, elevated body temp, increase creatine phosphokinase
46
What occurs during fight/flight response?
eyes dilate, bronchioles dilate, tachycardia, vasodilation, stop GI tract, liver breaks down glycogen for fuel
47
What are alpha 1 receptors responsible for?
vasoconstriction, increased peripheral resistance, increased BP, Mydriasis, increased closure of bladder sphincter
48
What are alpha 2 receptors responsible for?
Inhibit norepi release, inhibit ACh release, inhibit insulin releasea
49
What are B1 receptors responsible for?
Tachycardia, increased lipolysis, increased myocardial contractility, increased renin release
50
What are B2 receptors responsible for?
vasodilation, bronchodilation, increased muscle and liver glycogen breakdown, increased release of glucagon, relaxed uterus
51
What are B3 receptors responsible for?
Lipolysis
52
What is body's response to Norepi?
It's a pressor so pressure increases and HR reflex causes HR to go down. B1 only
53
What is body's response to Epi?
B2 is dominant. Pressure drops, HR reflex is to increase HR. Alpha 1 - vasoconstriction leads to drop in HR. Lots of epi, get Alpha 1 effect. Less, get B2 response.
54
What is the renal dopamine dose
1. Renal - Dopamine receptor agonist, decrease TPR (low dose)
55
What is the cardiac dopamine dose
2. decrease in TPR in renal and splachnics, but increase BP with mild increase in HR (intermediate dose). Becomes a B1 agonist
56
what is pressor dopamine does
3. High dose. Similar to norepi - big increase in pressure with little decrease in HR. Becomes alpha 1 agonist. Adverse effect can be hypertension, arrthymias
57
What is isoprotenol?
Non-selective beta agonist. Decreases BP, increases HR. Used as a bronchodilator when inhaled. If given through IV, temporary cardiac stimulant in Heart block and shock. Can also reduce pulmonary hypertension.
58
What are therapeutic uses of alpha 1 agonists?
``` TORN: T - topical hemostat O - ocular decongestant R - Raise BP N - nasal decongestant ```
59
What are therapeutic uses of Alpha 2 agonists?
2 A's - decrease aqueous humor production (because of decrease in ACh), Anti-hypertensive (because of norepi block)
60
What are therapeutic uses for Beta 2 agonists?
Increase HR, increase contractility
61
What are therapeutic uses of B2 agonists?
Lung drugs - Asthma, COPD, Delays Lab (relaxes uterine muscles), Increases HR, Increases force of contraction, decreases pulmonary resistance
62
What type of receptors do Alpha 1 use?
Gq - IP3 to DAG
63
What receptors use Gs - cAMP system
B1, B2, and dopamine
64
What receptors use Gi - cAMP system
Alpha 2, inhibit cAMP
65
What are cholinergic muscarinic receptors?
DAG - IP3
66
What are cholinergic nicotinic receptors?
Ion channel
67
What are epi, norepi, and dopamine metabolized?
MAO and COMT
68
What is epi used to treat?
bronchospasm, hypersensitivity reactions, topical hemostatic, anaphylactic shock, decrease IOP, in ACLS (cardiac rhythm, PEA, Vfib, Vtac)
69
Why is norepi dangerous to use?
such a strong pressor, can lead to necrosis if fluid drips on skin
70
What is dobuatmine used for?
Non-selective B agonist with some alpha 1 action. Increases contractility with no increase in HR. Slight decrease in TPR.
71
What is phenylephrine?
high alpha 1 affinity, increases pressures, reflex bradycardia. Uses: decongestant, pressor, vasoconstrictor with local anesthetics, mydriatic with little cycloplegia (paralysis of ciliary muscle)
72
How does pheylephrine work?
As an alpha 1 receptor agonist, it increases vasoconstriction of vessels (nasal vessels causes reduction in mucous production) and topical hemostat (vasoconstrict, less bleeding)
73
What is the fxn of Methoxamine and Metaraminol?
alpha receptor agonists, increase in BP with marked reflex bradycardia
74
What are some commonly used alpha receptor agonists used for nasal decongestant?
tetrahydrozline, naphazoline, oxymetazoline. ZOLINE
75
What are side effects of non-selective alpha agonists?
Initially hit Alpha 1s and cause vasoconstriction, but Alpha 2s dominate and cause vasodilation since alpha 2s block release of epi (pressor) (CNS effects lead to widespread BP drop).
76
What are three examples of non-selective alpha agonists
Clonidine, Guanabenz, Guanfacine
77
What selective alpha 2 agonists are used for wide angle glaucoma?
Apraclonidine Brimonide (block ACh release, decreases aqueous humor production)
78
What does terbutaline do?
beta 2 agonist, delays labor
79
What drugs are short-acting bronchodilators (up to 4 hours)
IF MAP: Isoetharine, Fenoterol, Metaproterenol, Albuterol, Pirbuterol (OL)
80
What drugs are long-acting bronchodilators (up to 12 hours)
Salmeterol Formoterm Salmon on the Farm
81
Why is it dangerous to take MAOI and eat cheese and drink beer?
MAOI inhibitors block reuptake of Catecholamines, leading to increase in action. Tyramine competes with Norepi for uptake, so tons of norpei gets left in the synaptic cleft. Leads to Vasoconstriction.
82
What is Ephedrine, Pseudoephedrine?
mixed acting with many actions, increases HR, contractility, BP, bronchodilates, myrdiasis, active nasal decongestant. Adverse: urinary incontinence
83
What do amphetamines, methamphetamine do?
promotes NE release, urinary retention, bronchodilation. Increases BP. Used for anuresis and as a diet aid
84
MAOIs?
Antidepressents. Goals is to keep seratonin and dopamine in the synaptic cleft
85
What inhibits neuronal uptake of catecholamines besides MAOIs
cocaine and trycyclic antidepressents
86
What are side effects and why?
reduced peripheral flow, rebound nasal congestion (receptor desensitization) Photophobia (mydriaisis) Urinary retention (sphincter tight)
87
What are contraindications to alpha agonists and why
CI in patients with glaucoma (myrdiasis causes radial contraction of eye leading to narrow angle glaucoma - block that gosh darn canal of schlemm), diabetes (alpha 2s decrease insulin), and hypertension (alpha 1 agonist)
88
Side effects of Beta agonists?
cardiac arrhythmias (B1 increases SA node firing) Anginal pain (increased contractility requires more O2) Tremors/Nervousness (increases symp resp) Tachycardia (decrease in BP leads to increase in HR if B2 are activated)
89
What are contrainidcations of Beta agonists
Angina (heart working harder, needs more O2), hyperthyroidism (increases HR too), diabetes (increased glycogenolysis means lots of sugar)
90
What do alpha 1 blockers treat?
Hypertension, urinary retention due to BPH
91
Why is phenoxybenzamine and what is used to treat?
LONG acting, Alpha 1 blocker, vasodilation with reflex increase in CO and HR. Little bit of action on A2s. Tx: Hypertension due to pheochromocytoma, BPH-related urinary retention. Side effect: orthostatic hypotension
92
Phentolamine is what and what does it treat?
It is shorter acting than phenoxybenzamine, and inhibits alpha 2 as well as alpha 1. histamine like action. Given paretnerally. Tx: hypertension, BPH-related urinary retention. Also see increase gastric HCl secretion
93
What do the selective A1 receptor blockers have in common in their name?
SIN. Prazosin, terazosin, trimazosin, doxazosin, Alfuzosin
94
What do A1 receptor blockers treat
Regular old hypertension and urinary retention from BPH. Loosen that sphincter. No marked increase in HR. Give first dose at night due to postural hypotension.
95
What is Prazosin + Alprostadil?
Bomb treatment for erectile dysfunction. Alpha 1 mediates ejaculatory response, and alprostadil causes dilation for erection.
96
What is Yohimbine?
Alpha 2 blocker to treat ED. "Yo, I got a Boner" Enhances release of ACh leading to POINTING da PENIS.
97
What do Beta receptor blockers names END with?
OLOL. Because one laughs out loud on beta blockers.
98
How do beta blockers work?
treat hypertension by decreasing cardiac output, inhibiting renin release and reducing angiotensin. They also prevent NT release in CNS. Treat angina by decreasing O2 demands and used as antiarrythmic to treat Afib. Tx glaucoma by inhibited aqueous humor production.
99
What is local anesthetic action?
This occurs with beta blockers that because they block sodium channels. These can treat arthymias and also increase depression.
100
Which drugs have local anesthetic action?
Labetalol, metoprolol, pindolol, propranolol
101
What is partial agonist activity with beta blockers?
Act as beta agonists for B2s. Thus, you can give these drugs to asthmatics.
102
What are the drugs with partial agonist activity (beta blockers)
Labetalol, Pindolol.
103
What is unique about propanolol.
This beta blocker has local anesthetic action and can be used for treating arrthymias. Complete oral absorption. 70% first pass effect.
104
What is unique about nadolol?
excreted by kidneys metabolicaly unchanged. No CNS action.
105
What is unique about Timolol?
5-10x more potent than propranolol. Large first pass effect. ALso used in chronic wide angle glaucoma
106
What is unique about timolol
blocks B1 cardiac stimulation, significant first pass extraction.
107
What is unqiue about nebivolol
selective beta 1 blocker with direct vasodilation properties (augments NO in vascular smooth muscle)
108
What do Labetalol and carvedilol do?
Alpha 1 blockers, Beta 1 blockers with partial agonist activity for B2 (asthmatics can use it). Blocks NE uptake, well absorbed, Tx: hypertension and pheochrymocytoma HT.

Pharm Block 1 (5 decks)

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