Drugs from every unit in random order Flashcards
(234 cards)
1
Q
Methotrexate pharmacodynamics
A
Act on specific enzymes
1
Q
Propranolol
A
Tx: arrythmias (Class II)
Mech: B1 blocker
Decreases pacemaker firing rate
SE:
- Bradycardia
- Hypotension
- B2 effects-asthma
2
Q
Niacin
aka Vit B3
aka Nicotinic acid
A
Tx: Hyperlipidemia
Mech:
- Inh. enzyme essential for VLDL synth
- May also bind to receptor that decreases VLDL synth
Effects:
- Decrease VLDL
- Increase HDL–strongest increase of any drug
SE:
- Cutaneous flushing and itching (prevented by aspirin)
- Increase uric acid–>gout
- Increase incidence of diabetes
3
Q
Calcium channel blockers
A
“-ipine”s
Inhibit Ca influx into vascular smooth m
Prevent vasoconstriction
SE:
- Heartburn
- May worsen heart failure
3
Q
Hydralazine
A
Act directly on smooth muscle
Arterial vasodilator
Increase in cGMP→relaxes smooth m
SE:
- Slow acetylators→lupus like syndrome
4
Q
Acetazolamide
A
Carbonic anydrase inhibitors (enzyme inhibitor)
Inhibits HCO3- resorption in PCT
Short term effect
Not used primarily as diuretic
Other uses:
- Treats open angle glaucoma
- Mountain sickness (by lowering CSF volume)
- Epilepsy
- May be due to pH in CNS
4
Q
Infliximab pharmacodynamics
A
Act on specific enzymes
4
Q
Anagrelide
A
Tx: Anticoagulant
Mech: Platelet inhibitor
Platelet count reducer
Decreases platelet formation, maturation, and #
4
Q
Antipsychotic drugs used to treat mania
A
Phenothiazine
Haloperitol
Benzos
5
Q
Lidocaine
A
Tx: arrythmias (Class Ib)
*also LA
Mech: Na channel blocker
Route: Given IV
Kinetics: First pass effect
Toxicity: Low
SE:
- Less likely to cause arrythmias but can enter CNS
- Tremors
- Seizures
7
Q
Mannitol
A
Osmotic diuretic
Not metabolized
Given IV
Mech: Draws H20 into tuble and is excreted w/ H20
Clinical use: Used to maintain renal flow after renal damage
Decreases intracranial pressure
8
Q
Cyclopentolate
A
Antimuscarinic agent
Blocks muscarinic receptor
Used to dilate pupils
8
Q
Inhibitors of Na transport in DCT and collecting tubule mech
A
K sparing diuretic
Prevent Na from getting into the exchanger by blocking Na ion channel
-Effects more rapid and predictable than spironolactone
9
Q
Minoxidil pharmacodynamics
A
Agents that act on ion channels
9
Q
Phenobarbital
A
Tx: All seizures EXCEPT petit mal
Class: Barbituate
Mech: Act. GABA
SE:
- Sedation
- Induces P450
10
Q
Topiramate
A
Tx: Partial seizures
Mech: Act. GABA
11
Q
Sarin
A
Nerve gas-direct cholinergic agonist
Irreversible AChE inhibitors
11
Q
Pralidoxime
A
If given early can reduce any perm. damage caused by organophosphate AChE inhibitors
11
Q
Sotalol
A
Tx: arrytmhias (Class III)
Mech: K+ channel blocker
Also a beta blocker
11
Q
Argatroban
A
Tx: Anticoagulant
Peptide from hirudin-diff structure, similar mech
Clinical use: when patient has HIT
Skin grafts and reattaching body parts
Route: Injection
11
Q
Fomepizole
A
Specific inhibitor of alcDH
Prolongs effects of alcohol
12
Q
Aldosterone antagonists
A
K sparing diuretics
Spironolactone
Eplerenone
12
Q
Insulin
A
Agents that act on cell membrane receptors
13
Q
Inhibitors of Na transport in DCT and collecting tubule
A
Triamterene
Amiloride
13
Other tx of bipolar
Most are antiseizure:
* Valproic acid
* Carbamazepine
* Limotripene
Acetazolamide
Aripripazole-anti-psychotic
14
Lamotrigine
Tx: **Partial seizures**
Mech: Inh. Na
15
Diazoxide
*Acts directly on smooth muscle*
Opens K channels→hyperpolarization
Inhibits insulin release from B cells in pancreas
16
Aliskiren
Renin inhibitor
SE:
* Fetal damage
* Diarrhea
* Cough
* Angioedema
17
Procaine pharmacodynamics
Agents that act on ion channels
17
High ceiling diuretics
Furosemide, ethacrynic acid, bumetanide, torsemide
* Orally or parenterally
17
Specific B1 receptor blockers
"olol"s
Metoprolol
Acebutolol
Alprenolol
Atenolol
Esmolol
Betaxolol
Nebivolol
These decrease HR
17
High Ceiling diuretics mechanism
Mech of action:
* Inhibit Na and Cl resorbtion from Asc. loop of Henle
More efficacious than thiazides
17
Mirtazapine
Antidepressant
18
Methylxanthines
Caffeine
increase glomerular filtration rate
19
ACE inhibitors
"-pril"s
ACE responsible for A1→A2
ACE responsible for bradykinin breakdown
Leads to decreased aldosterone secretion
SE:
* Rash
* Dry cough that cant be treated with suppressants
* Angioneurotic edema-swelling of nose, throat, resp tract
* Taste alteration
* Fetal damage
20
Aldosterone antagonists clinical use
1. Used w/ other diuretics to prevent K loss
2. To treat excess aldosterone production
21
Rocuronium
Antinicotinic agent
non-depolarizing neuromuscular blockers
Most common one
21
Non-depolarizing neuromuscular blockers that are antinicotinic agents are derived from?
curare
21
Fluvoxamine
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
22
Duloxetine
Third Generation Antidepressant
Mech: SNRIs
Inhibit reputake of 5HT and NE
\*Third generations have the -faxine drugs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Cardiovascular stimulation
\*SE same as 2nd gen +cardio stim.
23
Aldosterone antagonists mech
Blocks aldosterone receptor
Aldosterone is responsible for synth of Na-K exchanger
Takes days to be effective
24
Heroin
Narcotic analgesic- semisynthetic
Originally to cure morphine addiction
5x stronger than morphine
25
Agents that activate B2 receptors
"Nols and rols"
Metaproterenol
Terbutaline
Fenoterol
Albuterol
Tx: asthma
Causes bronchodilation
25
Olestra
Fake fat
SE: Butt leakage
25
Orlistat
Tx: Hyperlipidemia
Mech: Inh GI and pancreatic lipase
Decrease fat absorption from gut
SE: Loose stool
26
Vorapaxar
Tx: Anticoagulant
Mech: *Platelet inhibitor*
Thrombin receptor blocker on platelet
SE: Use carefully w/ pts w/ history of intracranial bleeding
27
Cocaine pharmacodynamics
Acts on transport systems
29
Bumetanide
High ceiling diuretics
Orally or parenterally
_Mech of action:_
Inhibit Na and Cl resorbtion from Asc. loop of Henle
More efficacious than thiazides
_Clinical use:_
Pts who dont respond to thiazides
Life threatening edema (pulmonary or cerebral)
Compromised renal fxn
_Side effects:_
Dehydration
Hypokalemia
---Used w/ K supplements or K sparing diuretics
Increased Ca excretion→Hypocalcemia
Decreased uric acid excretion→gout
Auditory nerve damage esp. if used w/ other ototoxic agents
30
Paroxetine
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
30
Phenytoin
Tx: Gran mal and others NOT petit mal
Mech:
* Inh. Na channels in brain
* Slows recovery rate of neuron
* Generally not a CNS depressant
Pharmakokinetics:
* Low TI
Toxicity:
* Acute
* Resp. depression
* Cardiovascular collapse
* Nausea
* Ataxia
* Chronic
* Gingival hyperplasia
* Vestibular effects
* Diplopia
* Ataxia
* Blurred Vision
* Some sedation
* Teratogenic-fetal hydantoin syndrome
* Life threatening rash-Stevens Johnson syndrome
31
Lacosamide
Tx: **Partial seizures**
Mech: Inh. Na
32
Fenoldopam
Activate D1 receptors
Given IV for HT emergencies
32
Dobutamine
Tx: CHF
Class: Inotropic agents
Mech: Beta1 agonist
Effects: Increase force of contraction
32
Isocarboxazid
Antidepressant-MAO inhibitor
Mech: Irreversibly inhibits metab of NE and 5HT (via inhibition of MAO)
Kinetcs: Slow onset
Toxicity:
Insomnia
Agitation
Hallucination
Seizure
Liver toxicity
Weight gain
Hypotension
Great increase in likelihood of suicide in children
Drug interactions:
Indirect acting amines→Hypertensive crisis
Some foods contain tyramine (smoked foods, aged cheeses, wine)
33
Atropine
Antimuscarinic agent
Blocks muscarinic receptor
Lasts 7-10 days
33
Aldosterone antagonists SE
* hyperkalemia
* Spironolactone is a steroid and can have anti-androgenic effect (breast growth,etc)
* Eplerenone-fewer interactions w/ steroid receptors
35
Neostigmine
Indirect cholinergic agonist
Lasts for several hours
Inhibit AChE
36
"-xaban"s
Tx: Anticoagulant
Mech: Factor Xa inhibitor
*Think -_xaban_=**_Ban_**s factor _Xa_*
Route: Oral
Kinetics: Rapid onset
SE: Bleeding after spinal tap or spinal injurty
36
Pregabalin
Tx: **Partial seizures**
Mech: Acts on Ca channels
37
Naphazoline
Adrenergic agonist
Activates alpha1 receptors
Tx: congestion
Taken intranasally
37
38
Desvenlafaxine
Third Generation Antidepressant
Mech: SNRIs
Inhibit reputake of 5HT and NE
\*Third generations have the -faxine drugs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Cardiovascular stimulation
\*SE same as 2nd gen +cardio stim.
40
Epinephrine
Works on all adrenergic receptors
Causes increased HR, etc. etc.
40
Dipryridamole
Tx: Anticoagulant
Mech: Platelet inhibitor
Inhibits phosphodiesterase
Inh. enzyme that breaks down cAMP
Increased cAMP→Decrease platelet agg.
40
"**Poetin**" and "**Pegin**"
**Epoietin alfa**
**Darbepoietin**
**Peginesatide**
Tx: Anemia due to _chronic renal failure_ or _chemotherapy_
Toxicities: Due to excess RBCs
* Increase BP
* Increase clotting
* MI
* Stoke
41
Icosapent
Tx: Hyperlipidemia
Mech: Inhibit enzyme responsible for Trig synth
Not clear though
41
Levetiracetam
Tx: **Partial seizures**
Mech: Unknown
42
Edrophonium
Indirect cholinergic agonist
Doesn't last very long
Inhibit AChE
43
More selective B blockers
Metoprolol
Acebutolol
Atenolol
Betaxolol
Nebivolol
SE:
* Fewer CNS effects
* Bradycardia
* Fatigue w/ exercise
44
Tissue plasminogen activator (TPA)
Tx: Thrombolytic agent
(dissolve formed clots)
Mech:
* Urine plasminogen activator=Enzyme activator
* Plasminogen→plasmin
* Plasmin:
* hydrolyzes fibrin
* degrades fibrinogen
* degrades factors V and VII
Route: IV
SE: May prolong bleeding time
45
Venlafaxine
Third Generation Antidepressant
## Footnote
Mech: SNRIs
Inhibit reputake of 5HT and NE
\*Third generations have the -faxine drugs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Cardiovascular stimulation
\*SE same as 2nd gen +cardio stim.
46
Acamprosate
Decreased craving for ethanol
47
Ipratropium
Antimuscarinic agent
Blocks muscarinic receptor
47
Hirudin
Tx: Anticoagulant--found in leech saliva
Mech: Directly inhibits thrombin
*Enzyme inhibitor*
48
Diltiazem
Tx: Arrythmias except vent. arrythmias (class IV)
Mech: Ca channel blockers
Increase refractory period
49
Mipomersen
Tx: hyperlipidemia
Antisense oligonucleotide
Mech: Binds to mRNA of ApoB
Prevents Apo from being synth
*\*(Apolipoprotein)\*+cholesterol→VLDL*
Must be given by injection
49
Amiodarone
Tx: arrytmhias (Class III)
DOC for cardiac arrest--most effective anti-arrythmic
Mech: K+ channel blocker
Acts like all 4 classes of anti-arrythmic
SE:
* Potentially fatal pulmonary fibrosis
* Replaces lung tissue w/ fiber composites
* Liver damage
* Corneal deposits-optic neuritis
* Deposits in skin-blue/gray skin coloration
* GI upset
\*Iodine responsible for some deposits
50
Cimetidine pharmacodynamics
Agents that act on cell membrane receptors
51
Methadone
Narcotic analgesic- synthetic
Orally effective-liquid
Less euphoric
Given to wean off morphine
Same strength as morphine
52
Procainamide
Tx: All arrythmias (Class Ia)
* Also LA
Mech: Na channel blocker
* Like quinidine but does not get into CNS
* Quinidine:*
* *Depresses all mm fxn*
* *Anti-cholinergic effects (antivagal effects)*
* *\*Vagal innervation slows HR--Quinidine will speed it up*
SE:
* Lupus like syndrome in slow acetylators
53
Sufentanil
Narcotic analgesic- synthetic
500-600x stronger than morphine
55
Malathion
Insecticide-cholinergic agonist
Irreversible AChE inhibitors
56
Nitroprusside
*Acts directly on smooth muscle*
Drug of choice in hypertensive emergencies
Acts w/in seconds--given IV
Dilates art and veins→drop in BP
increases cGMP→relaxation
Rapidly degrades in soln into cyanide
57
Glyceryl Trinitrate (nitroglycerin) (GTN)
Tx: Angina
Mech:
GTN→NO→Act. guanylate cyclase→cGMP→vasodilation
Rapidly dilates all blood vessels, including coronary art.
Route: Given sublingually--1st pass effect
Effects last 30-60min
Rapid tolerance so cannot take continuously
SE:
* Hypotension
* Skin flushing
* Headache-opening blood vessels in brain, feel pulsing
\*Nitroglycerin is unstable and explosive in some conditions
58
High Ceiling diuretics SE
* Dehydration
* Hypokalemia
* Used w/ K supplements or K sparing diuretics
* Increased Ca excretion→Hypocalcemia
* Decreased uric acid excretion→gout
* Auditory nerve damage esp. if used w/ other ototoxic agents
59
Imipramine
First generation antidepressant
Tricyclic antidepressants
Mech: Inhibit NE reuptake
Act on multiple receptors
SE:
Most likely to cause SE
Sedation
Weight gain
Anticholinergic effect (dry eyes, dry mouth, constipation)
Cardiovascular effects
Arrythmias
Drop in BP (alpha1 block)
Orthostatic hypotension
60
"-rudin"s
**Bivalirudin**
**Desirudin**
Tx: Anticoagulant
Synthetic analogs of hirudin
Clinical use: when patient has HIT
Skin grafts and reattaching body parts
Route: Injection
61
Angina definition and general tx methods
Not enough BF to heart
Causes chest pain (m becomes anoxic)
We usually have chest pain after we work out b/c we need more O2
But if at rest it is unstable angina
Tx by increasing BF or decreasing O2 demand
Tx:
* Behavioral
* Diet
* Exercise
* Creates collateral circulation (more blood vessels) in heart
* Stop smoking
* Drugs
62
Zonisamide
Tx: **Partial seizures**
Mech: Inh. Na
64
Acetazolamide
Tx: Seizures
Mech: May increase CO2 in brain→Decrease activity
65
Vortioxetine
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
66
Hydromorphone
Narcotic analgesic- semisynthetic
10x stronger than morphine
"Dilaudid"
68
Clonidine
Central alpha-2 agonist
_SE:_
Depression
Drowsiness
Dry mouth
Impaired Ejac.
_Unlabeled uses:_
* Fibromyalgia-unspecified neuronal pain
* Insomnia
* Tourettes
* Opiate withdrawal
70
MAO inhibitors
**Tranylcypromine**
**Phenelzine**
**Isocarboxazid**
Mech: Irreversibly inhibits metab of NE and 5HT (via inhibition of MAO)
Kinetcs: Slow onset
Toxicity:
* Insomnia
* Agitation
* Hallucination
* Seizure
* Liver toxicity
* Weight gain
* Hypotension
* Great increase in likelihood of suicide in children
Drug interactions:
* Indirect acting amines→Hypertensive crisis
* Some foods contain tyramine (smoked foods, aged cheeses, wine)
71
Ticlopidine
Tx: Anticoagulant
Mech: *Platelet inhibitor*
ADP receptor blocker on platelet
SE:
* Neutropenia-loss of neutrophils
* Agranulocytosis
71
Gabapentin
Tx: **Partial seizures**
Mech: Act **GABA**
**_GABA_**pentin
72
Verapamil
Tx: Arrythmias except vent. arrythmias (class IV)
Mech: Ca channel blockers
Increase refractory period
73
Disopyramide
Tx: Arrythmias (Class Ia)
Mech: Na channel blocker
* Even stronger antivagal effects (than quinidine)
SE:
* Antimuscarinic effects (opposite of DUMBBELS)
* Wouldn't use w/ glaucoma pts
75
Tirofiban
_Tx_: Anticoagulant
_Mech_: *Platelet inhibitor*
Fibrinogen receptor blocker on platelet (GPIIB/IIIA receptor)
_Clinical use_: Decrease white thrombi
Used for coronary operation
_Route_: IV
_SE_: Thromobocytopenia
76
Torsemide
High ceiling diuretics
Orally or parenterally
_Mech of action:_
Inhibit Na and Cl resorbtion from Asc. loop of Henle
More efficacious than thiazides
_Clinical use:_
Pts who dont respond to thiazides
Life threatening edema (pulmonary or cerebral)
Compromised renal fxn
_Side effects:_
Dehydration
Hypokalemia
---Used w/ K supplements or K sparing diuretics
Increased Ca excretion→Hypocalcemia
Decreased uric acid excretion→gout
Auditory nerve damage esp. if used w/ other ototoxic agents
78
Sitostanol
Tx: Hyperlipidemia
Mech: Looks like cholesterol--blocks uptake
79
Muscarine
Direct muscarinic agonist
80
Propranolol pharmacodynamics
Agents that act on cell membrane receptors
80
"Osin"s
Alpha 1 blockers
Blocks alpha 1 receptor on vascular smooth m
Tx of hypertension and some specifically treat BPH
Based on the drugs he gave us:
\*\*If it ends in -azosin its for hypertension\*\*
\*\*If it ends in just -osin its used for BPH\*\*
SE
* First dose effect-rapid drop in BP→orthostatic (postural) hypotension
* Do not confuse w/ first pass effect
80
Cilostazol
Tx: Anticoagulant
Mech: Platelet inhibitor
Inhibits phosphodiesterase
Inh. enzyme that breaks down cAMP
Increased cAMP→Decrease platelet agg.
82
Vigabatrin
Tx: **Partial seizures**
Mech: Act **GABA**
Vi**_GABAtrin_**
84
Morphine pharmacodynamics
Agents that act on cell membrane receptors
86
Bethanechol
Direct muscarinic agonist
87
Combined alpha and beta blockers
Block alpha1, beta1, and beta2
Labetalol
Carvedilol
SE:
* Postural hypotension
* Dry mouth
88
Oxycodone
Narcotic analgesic- semisynthetic
Partial agonist-available in oral form as oxycontin
0.5x as strong as morphine
89
Eptifibatide
_Tx_: Anticoagulant
_Mech_: *Platelet inhibitor*
Fibrinogen receptor blocker on platelet (GPIIB/IIIA receptor)
_Clinical use_: Decrease white thrombi
Used for coronary operation
_Route_: IV
_SE_: Thromobocytopenia
91
Digoxin
Tx: CHF
Class: Cardiac glycoside
* Naturally occuring (foxglove and milk weed)
* Produced as protection for plant
Route: orally
Kinetics: long T1/2
Mech:
* When m stimulated, small influx of Ca→causes release of Ca into cell from SR→contraction
* In order for m to relax after contraction, Ca must be removed (Na and Ca pumped out, K pumped in)
* Digoxin inhibits NaK-ATPase
* Na remains high in cell→prevents loss of Ca
* High conc of Na inhibits the Na-Ca exchanger
* Net result: Ca remains high
* High Ca→greater contractility
Effects:
* Increases duration of contractile response
* Stimulates vagus n
* Anti-arrythmic effects
SE:
* Cardiac arrythmias
* CNS effects
* Yellow-green tinting of vision
* Hallucinations
* Activation of chemoreceptor trigger zone→severe nausea
* Effects enhanced in hypokalemia
* Cardiac glycosides bind and K site
* If less K outside of cell, more effective
Digoxin poisoning treated w/ anti-digoxin anti-bodies
92
Non specific B1 and B2 blockers
Propanolol
Timolol
Levobunolol
Certeolol
Metipranolol
92
What induces the release of NE from nerve terminals?
Indirect acting amines:
Amphetamine, methamphetamine
Tyramine
Phenylpropanolamine
Pseudoephedrine
93
Spironolactone
K sparing diuretic
Aldosterone antagonist
_Mech:_
Blocks aldosterone receptor
Aldosterone is responsible for synth of Na-K exchanger
Takes days to be effective
_Clinical use_
Used w/ other diuretics to prevent K loss
To treat excess aldosterone production
_SE_
hyperkalemia
Spironolactone is a steroid and can have anti-androgenic effect (breast growth,etc)
Eplerenone-fewer interactions w/ steroid receptors
93
Omega 3 fatty acids
Tx: Hyperlipidemia
Mech: Inhibit enzyme responsible for Trig synth
Not clear though
95
Milnacipram
Third Generation Antidepressant
Mech: SNRIs
Inhibit reputake of 5HT and NE
\*Third generations have the -faxine drugs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Cardiovascular stimulation
\*SE same as 2nd gen +cardio stim.
95
Naltrexone
Narcotic analgesic antagonist
Opiate receptor blocker
97
Tranylcypromine pharmacodynamics
Act on specific enzymes
98
Methylnaltrexone
Narcotic analgesic antagonist
Opiate receptor blocker
99
Tramadol
Narcotic and SSRI
100
Heparin
_Tx_: Anticoagulant
_Mech_: Heparin binds to anti-thrombin (protease inhib) and increases its affinity for clotting factors by 1000x
Low doses: inhibits Xa, decreasing formation of thrombin
High doses: inhibits thrombin and irreversibly binds to IXa, XIa, and XIIa
Heparin inhibits clotting in vivo and in vitro
Activates lipoprotein lipases in blood
_Where we get it:_ located in mast cells
Harvest it from cow lung and pig intestines
Strong neg charge
Not synthetic-each batch tested individually
_Pharmacokinetics_: IV or subQ
Too large to be absorbed in GI tract or pass placenta
Not risk free in pregnancy though
Immediate onset--T1/2=1 hour
Degradation via heparinase
Can bind to variety of proteins so dose response in unpredictable
_Toxicity: _
* Generally non toxic
* Major danger is bleeding
* Overdose treated w/ protamine sulfate
* Strong pos charge binds w/ strong neg of heparin
* Long term use can lead to
* Osteoporosis-act. osteoclasts
* Thrombocytopenia-loss of platelets
* HIT-heparin induced thrombocytopenia
* Hypersensitivity-rare but we are injecting animal products
101
Demecarium
Indirect cholinergic agonist
Lasts for several hours
Inhibit AChE
103
Quinidine
Tx: All arrythmias (Class Ia)
Mech: Na channel blocker
* Depresses all mm fxn
* Anti-cholinergic effects (antivagal effects)
* \*Vagal innervation slows HR--Quinidine will speed it up
SE:
* GI
* Nausea and vomiting
* Anorexia
* CNS
* Tinnitus
* Alterted color vision
104
Thiazide diuretics SE and other effects
Other effects:
* Cause direct vasodilation
* Often initial drugs for hypertension
* Decrease Ca excretion
Side effects:
* Hypokalemia
* Lose K due to Na-K exchanger
* Increase in serum LDL and triglycerides (atherosclerosis)
* Decrease uric acid secretion→gout
* Inhibit insulin secretion
* Contain sulfur ions-may cause allergens
105
Third Generation antidepressants
**Venlafaxine**
**Desvenlafaxine**
**Duloxetine**
**Milnacipram**
Mech: SNRIs
Inhibit reputake of 5HT and NE
\*Third generations have the -faxine drugs
SE:
* GI upset
* Nausea
* Insomnia
* Headache
* Decreased libido
* Cardiovascular stimulation
\*SE same as 2nd gen +cardio stim.
107
Rufinamide
## Footnote
Tx: **Partial seizures**
Mech: Inh. Na
108
Metoprolol
Tx: arrythmias (Class II)
Mech: B1 blocker
More selective
SE:
* Bradycardia
* Hypotension
110
Fondaparinux
Tx: Anticoagulant
Synthetic heparin like drug
T1/2=17 hrs
Acts only on Xa
Can cross placenta
Can't bind protamine
Given SubQ
111
Prazosin
Adrenergic antagonist
alpha1 receptor blocker
Tx: hypertension
112
Fluoxetine
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
113
Amiloride
K sparing diuretic
Inhibitors of Na transport in DCT and collecting tubule
_Mech_:
Prevent Na from getting into the exchanger by blocking Na ion channel
-Effects more rapid and predictable than spironolactone
_SE:_
Hyperkalemia
114
Iomitapide
Tx: Hyperlipidemia
Mech: Inh assembly of VLDL in liver
*Apolipoprotein+cholesterol→(X)→VLDL*
Enzyme for assembly is also a transporter
SE: hepatotoxicity
115
Mexiletine
Tx: arrythmias (Class Ib)
Mech: Na channel blocker
Clinical use:
* Emergency tx of ventricular arrythmias
* Tx of ventricular tachycardia
Like lidocaine but can be given orally
116
Warfarin
Tx: Anticoagulant
Mech:
* Vit K analog--\***_K_**oagulation\*
* Inhibits enzyme that allows vit K to be recycled
* Leads to vit K deficiency
* Vit K is essential for factors 7, 9, 10 and prothrombin
* Works indirectly-doesn't directly block clotting cascade
Route: Oral
Pharmacokinetics:
* Factor T1/2s (hrs)
* VII--6
* IX--24
* X--40
* II--60
* So 5-6 T1/2s for 99% to be gone
* 30-36 hrs
* So initial onset is 24+ hours
* Metabolism
* P450
* Lots of drug interactions
* Phenytoin/barbituates vs grapefruit juice, etc.
* Diet interactions
* Lots of Vit K in green veggies
Toxicity:
* Overdose-tx w/ Vit K
* Hemorrhage
* Can pass placenta-preg. category X
116
118
First Gen Antidepressants
**Impiramine + Amitryptyline**
Tricyclic antidepressants
Mech: Inhibit NE reuptake
Act on multiple receptors
SE:
* Most likely to cause SE
* Sedation
* Weight gain
* Anticholinergic effect (dry eyes, dry mouth, constipation)
* Cardiovascular effects
* Arrythmias
* Drop in BP (alpha1 block)
* Orthostatic hypotension
119
Echothiophate
Indirect cholinergic agonist
Lasts for 100s hours
Phosphorylates AChE
120
Heparin pharmacodynamics
Act on specific enzymes
122
Pancuronium
Antinicotinic agent
non-depolarizing neuromuscular blockers
123
Inhibitors of Na transport in DCT and collecting tubule SE
Hyperkalemia
124
Nicotine
Direct nicotinic agonist
126
Succinylcholine
Direct nicotinic agonist
Antinicotinic agent-Depolarizing neuromuscular blocker
Long duration of action compared to acetylcholine
Initially activates receptor, eventually muscle hyperpolarization then paralysis
127
Calcium chelators
Citric acid (in blood transfusion bags(
ADTA
EGTA
Tx: Anticoagulants
Mech: Chelate Ca
Remove Ca from clotting cascade (4 steps need Ca)
We don't give these to people b/c Ca is involed w/ lots of mechanisms
128
Deferoxamine
Tx: Acute iron OD
Mech: Iron chelator
*_De_-_Fer_-oxamine*
***_De_**toxes **_Fer_**rous overdose*
130
Dabigatran
Tx: Anticoagulant
Mech: Direct thrombin inhibitor
*Enzyme inhibitor*
Route: Oral
Kinetics:
* Prodrug
* Onset w/in 1 hr
* P450 inhibitor may impact
SE-hemorhhage
131
Furosemide
High ceiling diuretics
Orally or parenterally
_Mech of action:_
Inhibit Na and Cl resorbtion from Asc. loop of Henle
More efficacious than thiazides
_Clinical use:_
Pts who dont respond to thiazides
Life threatening edema (pulmonary or cerebral)
Compromised renal fxn
_Side effects:_
Dehydration
Hypokalemia
---Used w/ K supplements or K sparing diuretics
Increased Ca excretion→Hypocalcemia
Decreased uric acid excretion→gout
Auditory nerve damage esp. if used w/ other ototoxic agents
133
How do anticancer drugs work?
Binds non-specifically to large molecules
135
Perampanel
Tx: **Partial seizures**
Mech: Blocks glutamate
136
Ethosuximide
Tx: DOC for **petit mal** seizures
Mech: Inhibit Ca channels in CNS
SE:
* GI upset
* Drowsiness
137
Alprostadil
Tx: ED
Injectable prostaglandin (PGE1) leads to vasodilation when injected directly into penis
138
Lithium
Tx: **Mania**
Used prophylactically--5-7 day onset
Cheap-can't patent it
Given orally
Low TI=2
Mech:
* Alter glutamate metabolism
* Decrease NE release
* May alter 5HT
SE:
* Short term
* Tremors
* Increase thirst
* Increase urine prod. (block effects of ADH)
* Edema
* Weight gain
* Nystagmus
* Long term
* Renal damage
* Hypothyroidism
Toxicity:
* Nausea
* Delirium
* Coma
* Dangerous w/ kidney disorders
139
Amitriptyline
First generation antidepressant
Tricyclic antidepressants
Mech: Inhibit NE reuptake
Act on multiple receptors
SE:
Most likely to cause SE
Sedation
Weight gain
Anticholinergic effect (dry eyes, dry mouth, constipation)
Cardiovascular effects
Arrythmias
Drop in BP (alpha1 block)
Orthostatic hypotension
140
Fenofibrate
Tx: Hyperlipidemia
Mech: Bind to PPAR-peroxisome proliferation acting _receptor_
Effects
* Increase transcription of LPLase
* Decrease VLDL
* Decrease Trig.
SE:
* GI upset-nausea, vomiting
* Can displace warfarin from plasma binding sites
141
Tapentadol
Narcotic and SSRI
143
Imitinib pharmacodynamics
Act on specific enzymes
144
Abciximab
_Tx_: Anticoagulant
_Mech_: *Platelet inhibitor*
Fibrinogen receptor blocker on platelet (GPIIB/IIIA receptor)
Monoclonal antibody
_Clinical use_: Decrease white thrombi
Used for coronary operation
Route: IV
_SE_: Thromobocytopenia
145
Phenelzine
Antidepressant-MAO inhibitor
Mech: Irreversibly inhibits metab of NE and 5HT (via inhibition of MAO)
Kinetcs: Slow onset
Toxicity:
Insomnia
Agitation
Hallucination
Seizure
Liver toxicity
Weight gain
Hypotension
Great increase in likelihood of suicide in children
Drug interactions:
Indirect acting amines→Hypertensive crisis
Some foods contain tyramine (smoked foods, aged cheeses, wine)
146
Agents that activate beta1 receptors
NE
Dobutamine
147
Aspirin pharmacodynamics
Act on specific enzymes
149
Fluoxetine pharmacodynamics
Acts on transport systems
150
Buproprion
Antidepressant
152
Aminocaproic acid
Tx: Hemostatic agent (enhance clotting)
Mech: Inhibits plasminogen activation
Enzyme inhibitor
Binds to plasminogen in plasma
Route: Oral or injection
153
How does ethanol work?
Binds non-specifically to large molecules
Protein denaturance
154
(Hydro)Chlorothiazide
Inhibits Na+ transport out of the DCT. H20 follows and both are excreted
High TI
works w/in 2 hours
Other effects:
Cause direct vasodilation
Often initial drugs for hypertension
Decrease Ca excretion
Side effects:
* Hypokalemia
* Lose K due to Na-K exchanger
* Increase in serum LDL and triglycerides (atherosclerosis)
* Decrease uric acid secretion→gout
* Inhibit insulin secretion
* Contain sulfur ions-may cause allergens
154
Codeine
Narcotic analgesic- narcotic analogs
Partial agonist-low anti-nociceptive effects
Given orally
Greater effect on coughing-anti-tussive effect
156
Nitroglycerin pharmacodynamics
Act on specific enzymes
157
Nifedipine pharmacodynamics
Agents that act on ion channels
158
"Choles- or coles-"
**Cholestyramine**
**Colestipol**
**Coleselevam**
Tx: Hyperlipidemia
Mech: Irreversibly _binds bile acids_ in gut→choles. excreted
Effects:
* Decrease circulating cholesterol
* Increase LDL receptor
Combine w/ statins for additional decrease in LPs
SE:
* No systemic SE-too big to be absorbed
* Can bind drugs
* Digoxin
* Oral anti-coagulants
* Decrease absorption of fat soluble vitamins
* GI upset-nausea
159
Adenosine
Tx:
* Arrythmias (Other class)
* Atrial Tachycardia
Mech:
* Binds to adenosine receptor
* Decreases firing rate of AV node
* Coronary vasodilator
Kinetics-Very short T1/2=10sec
161
Tranexamic acid
Tx: Hemostatic agent (enhance clotting)
Mech: Inhibits plasminogen activation
Enzyme inhibitor
Binds to plasminogen in plasma
162
Naloxone
Narcotic analgesic antagonist
Opiate receptor blocker
Naloxone-oxycodone combinations exist to make withdrawl easier
164
Alpha-methyl DOPA
Central alpha-2 agonist
Prodrug: metabolized to alpha-methyl NE
_SE:_
Depression
Drowsiness
Dry mouth
Impaired Ejac.
Hepatic dysfunction
165
Angiotensin receptor blockers
"-Artan"s
SE:
* Decrease secretion of aldosterone
* Fetal abnormalities
* All agents that alter angiotensin system
* Pregnancy risk X
167
Meperidine
Narcotic analgesic- synthetic
.5x as strong as morphine
No pupil constriction
168
Pilocarpine
Direct muscarinic agonist
169
Phenoxybenzamine
Adrenergic antagonist
alpha1 receptor blocker
Tx: hypertension
170
Citalopram
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
172
Propranolol
Tx of hypertension
Nonselective Beta blocker
Central and peripheral effects
Mech:
* Blocks B1 receptors on heart, prevents rise in HR
* Decreases renin secretion
* Renin converts Angiotensinogen→A1
SE:
* Into CNS→Depression
* Bradycardia→fatigue
* Impotence
* Lowers HDL, raises triglycerides
* Exacerbates asthma
174
Fentanyl
Narcotic analgesic- synthetic
80-100x stronger than morphine
175
High Ceiling diuretics clinical use
* Pts who dont respond to thiazides
* Life threatening edema (pulmonary or cerebral)
* Compromised renal fxn
176
Isosorbide dinitrate
Tx: Angina
Slow release nitrate formulation
Can be given orally
Slow enough that effects occur before 1st pass metabolism
178
"-grel"s
Tx: Anticoagulant
Mech: *Platelet inhibitor*
ADP receptor blocker on platelet
Same as ticlopidine-diff is pharmacokinetics: rapid onset, shorter T1/2
179
Escitalopram
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
180
Minoxidil
*Acts directly on smooth muscle*
Prodrug
Opens K channels in arterial smooth m, increased efflux→hyperpolarization
Very refractory px
SE:
* Hypertrichosis-hair growth
* Rogaine
* Discontinuation→hair loss
* Edema and pericardial effusion→cardiac tamponade
* Fluid in sac around heart
181
Reserpine
Tx of HT
Central and peripheral effects/effector of post-ganglionic neuron
Causes depletion of post ganglionic neuron nt (NE)→ No vasoconstriction
SE: depression, drowsiness, diarrhea
182
Morphine
Narcotic analgesic- narcotic analogs
Given parenterally due to first pass effect
183
Vilazodone
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
184
Carbamazepine
Tx: DOC for partial seizures
Mech: Inhibits on Na channels
Toxicity:
* Blurred vision + diplopia
* Drowsiness
* Fetal defects-spina bifida
* Aplastic anemia (abnormality of RBC)
* Induces P450
185
Ethacrynic acid
High ceiling diuretics
Orally or parenterally
_Mech of action:_
Inhibit Na and Cl resorbtion from Asc. loop of Henle
More efficacious than thiazides
_Clinical use:_
Pts who dont respond to thiazides
Life threatening edema (pulmonary or cerebral)
Compromised renal fxn
_Side effects:_
Dehydration
Hypokalemia
---Used w/ K supplements or K sparing diuretics
Increased Ca excretion→Hypocalcemia
Decreased uric acid excretion→gout
Auditory nerve damage esp. if used w/ other ototoxic agents
186
Ezetimibe
Tx: Hyperlipidemia
Mech: Blocks cholesterol transport
SE: Flatulence
187
Diazepam
Tx: Seizures
Class: Benzos
Mech: GABA
IV to treat status epilepticus
188
"-parin" drugs excluding heparin
**Enoxaparin**
**Dalteparin**
Tx: Anticoagulant
Low molecular wt heparins-Partially purified heparin
Longer T1/2=4 hrs
More effect on Xa than thrombin
Less osteoporosis and HIT
More predictable dose-response
(Smaller so don't bind as readily to lots of proteins)
More expensive
Not readily reversed by protamine sulfate
SE: spinal hematoma in pts who have had spinal tap or anesth.
189
Tacrine
Indirect cholinergic agonist
Alzheimer's tx
190
Omeprazole pharmacodynamics
Agents that act on transport systems
192
Tropicamide
Antimuscarinic agent
Blocks muscarinic receptor
Used to dilate pupils
193
Scopolamine
Antimuscarinic agent
Blocks muscarinic receptor
Lasts 3-7 days
194
Ezogabine
Tx: **Partial seizures**
Mech: Open K channel
195
Esmolol
Tx: arrythmias (Class II)
Mech: B1 blocker
More rapid onset of action
SE:
* Bradycardia
* Hypotension
* B2 effects-asthma
197
Remifentanil
Narcotic analgesic- synthetic
500-600x stronger than morphine
198
Thiazide diuretics
Chlorothiazide and hydrochlorothiazide
199
Sodium Valproate
Tx: All seizures including Petit mal seizures
Mech:
* Decrease GABA breakdown
* Increase GABA synth
* Act on Na and Ca channels
Toxicity:
* GI upset
* CNS sedation-tremors
* Potentially fatal hepatitis
* Fetal damage-drop in IQ
200
Sugammadex
Reverses block by rocuronium by binding directly
201
Phenylephrine
Adrenergic agonist
Activates alpha1 receptors
Tx: congestion
Taken intranasally
203
Tiagabine
Tx: **Partial seizures**
Mech: Act **GABA**
Tia**_gab_**ine
205
Ethanol as a diuretic
Mech: decrease release of ADH
207
Endothelin blockers
"-entan"s
Tx of pulmonary arterial hypertension
SE:
* Fetal damage
* Testicular atrophy
* Hepatic toxicity
208
Varenicline
Direct partial nicotinic agonist
Binds to receptor but does not fully activate it. Thus prevents others from binding.
Anti-smoking drug b/c binds but does not have effects of nicotine
209
Aspirin
_Tx_: Anticoagulant
_Mech_: *Platelet inhibitor*
COX (enzyme) inhibitor
Inhibits TXA2 synth
Decreases platelet aggregation
210
"-statin"s
**Lovastatin**
*Bunch of other -statins whose diff is pharmacokinetics*
Tx: _Hyperlipidemia_
Mech:
* Lovastatin is prodrug
* **HMG CoA reductase inhibitor**
* Rate limiting step in cell synth of their own cholesterol
* When cells can't make own cholesterol→increase in LDL receptors→increase LDL uptake
Effects:
* Decrease LDL (25%)
* Decrease VLDL synth
SE:
* Myositis (muscle pain)
* At worst→rhabdomyolysis (muscle breakdown)
* Liver toxicity
* Teratogenic--preg. category X
* Some memory loss
Kinetics-metab by P450
211
Alfentanil
Narcotic analgesic- synthetic
500-600x stronger than morphine
212
Triamterene
K sparing diuretic
Inhibitors of Na transport in DCT and collecting tubule
_Mech:_
Prevent Na from getting into the exchanger by blocking Na ion channel
-Effects more rapid and predictable than spironolactone
_SE:_
Hyperkalemia
213
Gemfibrozil
Tx: Hyperlipidemia
Mech: Bind to PPAR-peroxisome proliferation acting _receptor_
Effects
* Increase transcription of LPLase
* Decrease VLDL
* Decrease Trig.
SE:
* GI upset-nausea, vomiting
* Can displace warfarin from plasma binding sites
214
Nefazodone
Antidepressant
215
Second generation antidepressants
**Fluoxetine**
**Fluvoxamine**
**Sertraline**
**Paroxetine**
**Citalopram**
**Escitalopram**
*Vilazodone*
Mech: SSRIs
SE:
* GI upset
* Nausea
* Insomnia
* Headache
* Decreased libido
216
Sertaline
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
217
Prazosin pharmacodynamics
Agents that act on cell membrane receptors
218
Nifedipine
Tx: Arrythmias except vent. arrythmias (class IV)
Mech: Ca channel blockers
Increase refractory period
219
"-kinase"s
**Streptokinase**
**Urokinase**
Tx: Thrombolytic agent
(dissolve formed clots)
Mech:
* Urine plasminogen activator=Enzyme activator
* Plasminogen→plasmin
* Plasmin:
* hydrolyzes fibrin
* degrades fibrinogen
* degrades factors V and VII
Route: IV
SE: May prolong bleeding time
220
"-afils"
Sildenafil
Vardenafil
Tadalafil
Avanafil
Tx: ED
Mech:
* Inhibits type 5 cGMP phosphodiesterase
* Nitrates→NO→cGMP→smooth m relax
* cGMP degraded to 5'GMP via _type 5 cGMP phosphodiesterase_
* Relaxes arteries in corpus cavernosum→increase BF
SE:
* Slight drop in BP
* Do not use w/ alpha 1 blockers or nitrates
* Too much drop in BP
* Stroke
* MI (may be due to activity)
* Visual disturbances
* Impaired blue/green color discrimination
* NAION-some potential for damage to retina induced by cGMP PDE inhibitors
Metabolism: P450
221
Disulfiram
Inhibits acet.DH→buildup of acetaldehyde
Get severe hangover right away
222
Donepezil
Indirect cholinergic agonist
Alzheimer's tx
223
Clonidine
Adrenergic agonist
Activates alpha2 receptors
Decrease symp outflow from CNS
Tx: hypertension
Other analogs used for glaucoma (Decrease pressure)
224
Thiazide diuretics mechanism
Inhibits Na+ transport out of the DCT. H20 follows and both are excreted
High TI
works w/in 2 hours
225
Tranylcypromine
Antidepressant-MAO inhibitor
Mech: Irreversibly inhibits metab of NE and 5HT (via inhibition of MAO)
Kinetcs: Slow onset
Toxicity:
Insomnia
Agitation
Hallucination
Seizure
Liver toxicity
Weight gain
Hypotension
Great increase in likelihood of suicide in children
Drug interactions:
Indirect acting amines→Hypertensive crisis
Some foods contain tyramine (smoked foods, aged cheeses, wine)
226
alpha-methyl tyrosine
Tx of pheochromocytoma
Central and peripheral effects
Inhibits tyrosine kinase--preventing synthesis NE and epi
227
atracurium
Antinicotinic agent
non-depolarizing neuromuscular blockers
228
alpha-methyl NE
Adrenergic agonist
Activates alpha2 receptors
Decrease symp outflow from CNS
Tx: hypertension
Other analogs used for glaucoma (Decrease pressure)
229
Hydroxyurea
Mech: Increase formation of fetal Hb (does not sickle)
SE: Mutagenic
Pregnancy category D
230
Dronedarone
Tx: arrytmhias (Class III)
Mech: K+ channel blocker
Analog of amiodarone
Fewer SE-less efficacious
231
Physostigmine
Indirect cholinergic agonist
Lasts for several hours
Inhibit AChE
232
Eplerenone
K sparing diuretic
Aldosterone antagonist
_Mech: _
Blocks aldosterone receptor
Aldosterone is responsible for synth of Na-K exchanger
Takes days to be effective
_Clinical use_
Used w/ other diuretics to prevent K loss
To treat excess aldosterone production
_SE_
hyperkalemia
Spironolactone is a steroid and can have anti-androgenic effect (breast growth,etc)
Eplerenone-fewer interactions w/ steroid receptors
233
Homatropine
Antimuscarinic agent
Blocks muscarinic receptor
Used to dilate pupils
234
Tetrahydrozoline (Visine)
Adrenergic agonist
Activates alpha1 receptors
Tx: congestion
Taken intranasally
