Test 4 Flashcards
1
Q
MOA of Beta-Adrenergic Receptor Agonists
A
Stimulate Beta 2 receptors in the lungs –> increased ATP –> increased cAMP –> Relaxation in the lungs
2
Q
Therapeutic Effects of Beta Adrenergic Receptor Agonists
A
Bronchodilate, Inhibit bronchoconstricting mediators, increase mucus clearance
3
Q
MOA of non-selective Beta Adrenergic Agonists
A
Act on both beta 1 and beta 2 receptors in heart and lungs
4
Q
MOA of selective Beta Adrenergic Agonists
A
Act on just beta 2 receptors in lungs unless high doses
5
Q
Non-Selective Beta-Adrenergic Receptor Agonist Drugs
A
Epinephrine (Adrenalin, Primatene)
Terbutaline (Brethine)
6
Q
Epinephrine (Adrenalin, Primatine)
A
Non-Selective Beta-Adrenergic Receptor Agonist, SABA
7
Q
Terbutaline (Brethine)
A
Non-Selective Beta-Adrenergic Receptor Agonist, SABA
8
Q
Selective Beta-Adrenergic Receptor Agonist Drugs
A
Albuterol, Levalbuterol, Salmeterol, Formoteral
9
Q
Albuterol (Proventil, Ventolin)
A
Selective Beta-Adrenergic Receptor Agonist Drugs, SABA
10
Q
Levalbuterol (Xopenex)
A
Selective Beta-Adrenergic Receptor Agonist Drugs, SABA
11
Q
Salmeterol (Serevent)
A
Selective Beta-Adrenergic Receptor Agonist Drugs, LABA
12
Q
Formoterol (Foradil)
A
Selective Beta-Adrenergic Receptor Agonist Drugs, LABA
13
Q
SABA MOA
A
Onset 5 min, Duration 4-6h, rescue inhaler
14
Q
LABA MOA
A
Onset 30 min, Duration 12 h, maintenance inhaler, last choice
15
Q
What must you prescribe with a Beta Adrenergic Receptor Agonist?
A
Corticosteroid, Contra Indicated without
16
Q
Adverse effects of Beta-Adrenergic Receptor Agonists
A
Tachycardia, Decreased serum potassium, tremors, Tolerance
17
Q
Beta-Adrenergic Receptor Agonists DDIs
A
Adrenergic, beta blockers
18
Q
MOA Methalxanthines
A
Inhibit PDE which breaks down cAMP –> 5’-AMP. More cAMP leads to more relaxation in lungs. Increases mucus clearance.
19
Q
Clinical use Methylxanthines
A
Limited because of narrow therapeutic index. Maintenance therapy if you’ve tried everything else.
20
Q
Therapeutic Index of Methalxanthines
A
5-15
21
Q
ADE of Methalxanthines
A
Happen at any concentration. CNS = seizures, insomnia. Tachycardia, N/V, Tremors. Lots of DDI.
22
Q
Pharmokinetics of Methalxanthines
A
90% liver metabolism, 10% excreted unchanged by kidneys
23
Q
Methylxanthines
A
Theophylline - PO, Aminophylline - IV.
24
Q
Theophylline
A
PO. No mg to mg switching, Methylxanthine.
25
Aminophylline
IV, Methylxanthine
26
Anticholinergic Agents MOA
Compete with ACH at muscarinic receptor. Decrease vagal tone to airway which leads to bronchodilation.
27
Anticholinergic Uses
Inhalation only, treat acute asthma with a SABA because they have an additive effect.
28
What do you need to prescribe with an anticholinergic to treat acute asthma
SABA, additive effect
29
Corticosteroid MOA
Reduce markers of inflammation, decrease vascular congestion and cellular infiltration, improve beta 2 receptor sensitivity
30
Corticosteroid Therapeutic Effects
IV or PO (1-2 hrs vs 2wks), for acute use IV --> oral, for prevention use inhalation and dose based on severity.
31
Corticosteroid Inhallation ADE
Fungal infections in the mouth, wash mouth
32
Corticosteroid Systemic Short Term ADE
Hyperglycemic, Psychiatric
33
Corticosteroid Systemic Long Term ADE
Osteoporosis/fractures, HTN, poor wound healing, Adrenal suppression, myopathy, glaucoma
34
Corticosteroid DDI
Cushings and adrenal insufficiency reported with CYP inhibitors
35
What three classes/drugs lower seizure threshold?
Beta-Lactams (Imipenem), Buproprion, Meperidine
36
Sodium Channel Blockers MOA
Reduce Na+ influx which reduces neuron firing, prolongs the inactivation state of neurons and inhibits the release of excitatory amino acids
37
Class for Carbamazepine (Tegretol)
Sodium Channel Blocker
38
Carbamazepine Pharmicokinetics
- Highly protein bound
- Autoinduction
- Hepatic Metabolism with active metabolites
- Inducer of CYP34A
- Monitor Serum levels
39
Carbamazepine Theraputic Uses
Generalized tonic-clonic and partial
40
Carbamazepine ADE
CNS: Blurred vision, unsteady, headache, sedation. Nausea. Hyponatremia (SIADH)
41
Carbamazepine BBW
Blood dyscrasia and Derm (Steven's Johnson and TENS). Worse for Asians due to alleel.
42
Carbamazepine DDI
Inducer, displacement reactions
43
Oxcarbazepine (Trileptal) Class
Sodium Channel Blocker, analog of Carbamazepine
44
Oxcarbazepine (Trileptal) Pharmicokinetics
- Highly protein bound
- Not CYP450 Metabolized
- Eliminated by kidneys
- Inducer of CYP34A
- Initiate dose at 1.5x > Carbamazepine
45
How many times higher is an Oxcarbazepine (Trileptal) dose than a Carbamazepine dose?
1.5 times higher for Oxcarbazepine (Trileptal)
46
Oxcarbazepine (Trileptal) Theraputic Uses
Generalized tonic-clonic, partial
47
Oxcarbazepine (Trileptal) ADE
No BBW, SIADH
48
Oxcarbazepine (Trileptal) DDI
Inducer of 34A, reduced oral contraception
49
Eslicarbazepine Class
Sodium Channel Blocker, analog of Carbamazepine
50
Eslicarbazepine Clinical Application
Partial onset seizures
51
Eslicarbazepine Pharmacokinetics
- Highly protein bound
- Adjust for renal dysfxn
- Inhibits CYP 2C19, Induces CYP 34A
52
Eslicarbazepine ADE
No BBW, Derm rxn, hyponatremia, hepatotoxicity, reduces oral BC
53
Phenytoin (Dilatin) Class
Sodium Channel Blocker
54
Phenytoin (Dilantin) Types
Phenytoin Acid and Phenytoin Sodium - Sodium has 8% less phenytoin. NOT bioequivilent. Check levels when dosing
55
Phenytoin (Dilatin) Levels
Levels are given with bound + free. Free is usually 10% unless they have hypoalbumin (less is bound) or high urea and bilirubin which can knock it off. Can order "free" level
56
Phenytoin (Dilatin) Conditions that affect binding
Renal failure, liver failure, hypoalbuinemia (Major trauma, burns, nephrotic syndrome, malnutrition, surgery)
57
Phenytoin (Dilatin) Metabolism
Dose-dependent, Michaelis-Mentin or capacity limited metabolism. CYP450 interactions. 20% less clerance in the elderly
58
Phenytoin (Dilatin) Target concentrations
10-20 mcg (1-2 mcg free)
59
Phenytoin (Dilatin) Adjustments
Adjust for Albumin
60
Phenytoin (Dilatin) Treatment uses
Generalized tonic-clonic, partial
61
Phenytoin (Dilatin) Dose dependent ADE
>20 --> nystagmus, >30 ataxia, seizures, >40 --> lethargy or coma
62
Phenytoin (Dilatin) Hypersensitivity ADE
Rash, increased LFT, Fever
63
Phenytoin (Dilatin) Long Term ADE
Gingival Hyperplasia, Hirsuitism
64
Phenytoin (Dilatin) IV ADE
CV problems from propolene glycol in IV, Purple glove syndrome from extravision
65
Phenytoin (Dilatin) ADE
N/V/C, Decreased cognitive ability, Leukopenia, Thromboytopenia, Anemia
66
Phenytoin (Dilatin) DDI
Inducer of 3A4, Metabolized by 2C9/2C19, protein bound, tube feedings and antacids reduce availability, separate by 2 hr
67
Phenytoin (Dilatin) vs Fosphenytoin
Max infusion of Phenytoin is 50 (25 in elderly) vs 150 because Fosphenytoin has no propylene glycol. Phenytoin cannot be given IM, Fosphenytoin can.
68
Fosphenytoin vs Phenytoin doses
1.5 mg of fosphenytoin = 1 mg of phenytoin
69
Fosphenytoin (Cerebyx) Pharmokinetics
Prodrug of Phenytoin, converts in the blood. Can be IM or IV. Same ADE as Phenytoin minus the IV ADE.
70
Zileuton (Zyflo)
Leukotriene Modifer
71
Zileuton (Zyflo) MOA/ADE
Prevent leukotriene formation, Hepatotoxicity
72
Zafirlukast (Accolate)
Leukotriene Modifier
73
Montelukast (Singular)
Leukotriene modifier
74
Leukotriene Modifier MOA
Affect Leukotrenes which are potent constrictors produced from arachidonic acid. Affect LTC and LTD4.
75
Zafirlukast and Montelukast MOA
Receptor antagonists for LTD4
76
Leukotriene Modifier Uses
Maintenance therapy, alternative to corticosteroids, Prophylaxis and aspirin induced asthma
77
Leukotriene Modifier ADE
Headache, GI upset, CYP 450 Interactions
78
Monoclonal Antibody MOA
Inhibits IgE from binding to receptors on mast cells
79
Monoclonal Antibody ADE
Injection site rxn
80
Monoclonal Antibody Therapeutic uses
Moderate to severe allergy asthma not controlled by steroids
81
What should every asthmatic have on hand?
SABA, Beta-2 Rescue inhaler
82
What should every persistent asmathtic by eon?
Corticosteroid
83
Goals of COPD Therapy
Prevent disease progression, relieve sxs, tx and prevent acute exacerbations, smoking cessation
84
Long term management of COPD
Supplemental oxygen, regular tx with bronchodilators (Anticholinergics), inhaled corticosteroids
85
Acute COPD Exacerbations
SABA, Antibiotics (if not viral infection)
86
Most important part of smoking cessation
Set a quit date
87
Nicotine Replacement MOA
Maintain levels of dopamine over time, can be slowly decreased
88
Nicotine Replacement Cautions
Patients that are post MI, with arrhythmias or angina
89
Bupropion SR (Zyban) Mechanism of Action
Blocks the reuptake of dopamine
90
Bupropion SR (Zyban) Therapeutic Uses
Use with NR, first choice for depressed patients, well tolerated in patients with CV disease, delays weight gain, begin therapy 1-2 weeks before quit date
91
Bupropion SR (Zyban) Caution
Seizure disorders
92
Varenicline (Chantix) MOA
Selective for nicotine receptors, partial agonist, prevents full agoinst activity
93
Varenicline (Chantix) ADE
Serious neuropsychaitric symptoms such as agitation, depression, suicial ideation
94
Which Insulin should be cloudy
NPH
95
What do you use Rapid/Short acting insulin for?
Meal intake, elevated glucose, IM or IV
96
What do you use intermediate/long acting insulin for
Basal insulin needs, NOT to cover long meals, must be given IM
97
How much does 1 unit of insulin lower blood glucose?
50-100 mg/dL
98
How long do you wait before adjusting the dose?
24hr to prevent hypoglycemia
99
Insulin injection sites
Abdomen > buttocks > arm/leg. Exercise/rubbing.heat accelerates absorbtion
100
Treat Mild Hypoglycemia
Simple sugar (juice, candy, sugar_
101
Treat Severe hypoglycemia (Unconscious)
20-50 mL of 50% dextrose by IV. 1mg glucoagon subq or IM
102
Technosphere insulin
Dry, powder insulin. Dose at begining of meal. BBW for bronchoconstriction, not recommended for smokers
103
Lispro (Humalog)
Rapid acting insulin
104
Aspart (Novolog)
Rapid Acting insulin
105
Glulisine (Adventis)
Rapid Acting insulin
106
Rapid Acting Insulin
Onset 15-30min, Peak 1-2h, Duration 3-4h, Admin before meal, IV or SubQ, clear
107
Regular (Humulin R)
Short Acting Insulin
108
Short Acting Insulin
Onset 30 min, Peak 2-3h, Duration 4-6h, Admin 40-45min before meal, IV or SubQ, clear
109
NPH (Humulin N) and NPH (Novolin N)
Intermediate Acting Insulin
110
Intermediate Acting Insulin
Onset 2-4h, peak 4-8hr, duration 8-12hr, usually BID, Only SubQ, Cloudy
111
Glargine (Lantus)
Long Acting Insulin
112
Detemir (Levemir)
Long Acting Insulin
113
Insulin ADE
Hypoglycemia, Insulin allergy, Insulin resistance (Animal), Lipohypertrophy --> reduced absorbtion
114
Glipizide
Sulfonylurea
115
Glimepiride
Sulfonylurea
116
Glyburide
Sulfonylurea
117
Sulfonylureas MOA
Target Sulfonylurea receptor on beta pancreatic cell to force insulin to be released without needing glucose to be present
118
Sulfonylureas Use/Pharmikokinetics
Extended duration of action, DM 2, reduce dosing with hepatic impairtment
119
Sulfonylurea ADE
Hypoglycemia, Sulfa moity --> Derm (rash, photosensitivity), GI: N/V/LFTs, weight gain
120
Glipizide Preferred Use
Elderly, no renal excretion "Glip is Hip"
121
Glyburide Risks
50/50 renal and hepatic excretion, accumulates in pts with CrCl
122
Repaglinide (Prandin)
Meglitinide
123
Nateglinide (Starlix)
Meglitinide
124
Meglitinide MOA
Same as Sulfonylurea but no sulfa moity
125
Meglitinide uses
Preferable for those who skip meals, shorter duration of action, preferable for those with renal dysfunction
126
Meglitinide ADE
Hypoglycemia, weight gain, DDI: Inhibit CYP450
127
Metformin (Glucophage)
Biguanide
128
Biguanide MOA
Decrease hepatic glucose output, increase peripheral glucose utilization
129
Biguanide Uses
DM 2
130
Biguanide Advantages
Cause weight loss, decreaes triglicerides
131
Biguanide Contraindications
Men CrCL >1.5, Women >1.4, Hypoxia, Renal impairment, hepatic impairment, contrast materials all lead to lactic acidosis
132
Biguanide ADE
GI upset, bloating and flatulance, lactic acidosis
133
Acarbose (Pregose)
Alpha Glucosidase Inhibitor
134
Miglitol (Glyset)
Alpha Glucosidase Inhibitor
135
Alpha Glucosidase Inhibitor MOA
Inhibit brush border alphaglucosidases which slows down digestion of complex carbohydrates
136
Alpha Glucosidase Inhibitor ADE
Flatulence, Abd pain, diarrhea, CI in pt with GI disorders
137
Acarbose (Pregose) ADE
Increases LFTs
138
Rosiglitazone (Avandia)
Thiazolidinedione
139
Pioglitazone (Actose)
Thiazolidinedione
140
Thiazolidinedione MOA
Promote uptake of glucose into muscle/adipose. Decrease insulin resistance, increase insulin sensitivity, no effect on insulin secretion
141
Thiazolidinedione ADE
Hepatotoxicity and edema, fracture risk, caution in CHF patients and risk for ostoporosis
142
Pioglitazone (Actose) ADE
Risk for bladder cancer, CI in bladder cancer
143
Exenatide (Byetta), Ligalutide (Victoza), Albiglutide (Tanzeum), Dulaglutide (Trulicity)
GLP-1 Antagonists
144
GLP-1 Antagnosts MOA
Mimic Action of GLP-1. Stimulate insulin release, delay gastric emptying, suppress glucagon release. Recombinant form.
145
GLP-1 Antagonists Contraindications
CrCl
146
GLP-1 Antagonists ADE
N/V, Headache, **Pancreattitis
147
Sitagliptin (Januvia), Saxagliptin (Onglyza) Alogliptin (Nesina), Lingagliptin (Tradjenta)
DPP-4 Inhibitors
148
DPP-4 Inhibitors MOA
Inhibit DPP-4 Enzyme that breaks down GLP-1.
149
DPP-4 Inhibitors ADE
Adjust for renal dysfunction, Pancreatitis
150
What do you start a DM2 patient with very high glucose on first?
Insulin
151
What is the backbone of all HA1C treatments?
Metformin
152
Zosinamide (Zonegran)
Calcium Channel Blocker
153
Zosinamide (Zonegran) Pharmikokinetics
Low Protein Binding, PO only, Hepatic metabolism, kidney excretion
154
Zosinamide (Zonegran) ADE
CNS: Somnolence, Agitation, cognitive impairment, Renal Stones, Sulfa Moity
155
Lamotrigine (Lamictal)
Calcium Channel Blocker
156
Lamotrigine (Lamictal) Pharmikokinetics
Low protein binding, PO
157
Lamotrigine (Lamictal) ADE
BBW for skin rxn if patient is positive for allelle (TENS or SJS). DDI with Valproic acid (Adjust dosing)
158
Rufinaminde (Banzel)
Calcium Channel Blocker
159
Rufinaminde (Banzel) Pharmikokinetics
Hepatic metabolism, CYP Inducer
160
Rufinaminde (Banzel) ADE
Short QT interval, multi-organ hypersensitivity
161
Lascosamide (Vimpat)
Calcium Channel Blocker
162
Lascosamide (Vimpat) Pharmikokinetics
100% bioavailible PO, hepatic metabolism, renal elimination
163
Lascosamide (Vimpat) ADE
Prolong QT interval, heart block, no DDI
164
Valproate
GABAergic Agent
165
GABAergic Agent MOA
Increase the activity of the inhibitory neurotransmitter GABA in order to prevent and treat seizures
166
Valproate Pharmicokinetics
Many forms, stick to one. Highly protein bound. Inhibit CYP450**, Concentration 50-100 or higher if needed
167
Valproate ADE
BBW for hepatotoxicity, tetrogenaity and pancreatitis. Weight gain, thrombocytopenia, Hyperammonemia, Displacement reaction (Phenytoin), Increase Lamotrigine levels (Skin Rxn), CYP Inhibitor
168
Gabapentin
GABAergic Agent
169
Gabapentin Pharmikokinetics
Oral, renal elimination
170
Gabapentin ADE
CNS: Somnolence, dizziness, ataxia, emotional lability, agitation. No DDI. Withdrawl
171
Tigabine (Gabatril)
GABAergic Agent
172
Tigabine (Gabaril) Pharmikokinetics
Highly protein bound
173
Tigabine (Gabaril) ADE
Hallucinations/paranoia, Displacement DI
174
Vigabatrin (Sabril)
GABAergic Agent
175
Vigabatrin (Sabril)
MUST be an approved provider
176
Vigabatrin (Sabril)
BBW - Irriversible vision loss
177
Clobaxam (Onfi)
GABAergic Agent
178
Clobaxam (Onfi) Pharmikokinetics
PO, Highly protein bound
179
Clobaxam (Onfi) ADE
Benzo affects
180
PHENObarbitol
GABAergic Agent
181
PHENObarbitol Pharmikokinetics
PO only, Highly protein bound
182
PENTObarbitol
GABAergic Agent
183
PHENObarbitol ADE
Benzo affects
184
PENTObarbitol Pharmikokinetics
IV not PO
185
PENOTbaribol ADE
Benzo affects
186
What is the first drug you reach for with status epilipticus?
IV Benzos, IM Midazolam, PR diazepam
