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IPAP JUNIOR SEM. > PHARM III Drugs And Class And MOA > Flashcards

PHARM III Drugs And Class And MOA Flashcards

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1
Q

Cylcobenzapine

Class, MOA, and C/U

A

CNS Depressant Muscle relaxant
Antispamodic

MOA: Structurally related to tricyclic antidepressants (TCA); causes a depressant effect on serotonergic neurons; has strong anticholinergic and antihistamine properties

C/U: short term local muscle spasms, ineffective at Tx of cerebral palsy or spinal cord injury
(SHORT TERM 2-3 weeks)

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2
Q

Orphanadrine

Class? MOA?? C/U??

A

CNS Depressant Muscle relaxant
Antispasmodic

MOA: Analog of diphenhydramine

Antihistamine and anticholinergic properties

Has euphorigenic and analgesic properties; Full mechanism is unknown

C/U: Treatment of muscle spasm associated with acute painful musculoskeletal conditions
Used short term (2-3 weeks)

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3
Q

Carisoprodol

Class? And MOA? C/U?

A

CNS Depressant Muscle relaxant
Antispasmodic

MOA:
Blocks interneuronal activity and depresses polysynaptic neuron transmission

Metabolized to meprobamate, which has anxiolytic and sedative effects

C/U: Relief of discomfort associated with acute, painful musculoskeletal conditions in adults
Used short term (2-3 weeks)

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4
Q

Metaxalone

Class and MOA, C/U?

A

CNS Depressant Muscle relaxant
Anitspasmodic

MOA: unknown; associated with general depression of the nervous system

C/U: Relief of discomforts associated with acute, painful musculoskeletal conditions
Appears to cause less drowsiness than others

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5
Q

Tizanidine

Class and MOA, C/U?

A

A2 agonist muscle relaxant

MOA: centrally acting α2 agonist (~clonidine)

Reduces spasticity by increasing presynaptic inhibition of motor neurons

1/10 to 1/15 of the blood pressure lowering ability as clonidine

Clinical Use:
Muscle spasticity
Short acting agent

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6
Q

Baclofen

Class and MOA, C/U ?

A

GABA Agonist

Mechanism of Action:
Orally active GABA-mimetic agent at the level of the spinal cord

Presynaptic inhibition by reducing calcium influx and reduces the release excitatory transmitters in both the brain and the spinal cord

May also reduce pain in patients with spasticity by inhibiting the release of substance P in the spinal cord

Clinical Use:
Anti-spastic agent
Drug of Choice for Multiple Sclerosis (MS)
At least as effective as diazepam in reducing spasticity and causes less sedation
Does not reduce overall muscle strength

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7
Q

Diazapam

Class and MOA

A

GABA Agonist

Mechanism of Action:
Bind to specific high affinity sites on the cell membrane separate but adjacent to the GABA receptor (allosteric binding)

Enhancement of the INHIBITORY effect of GABA on neuronal excitability (increase chloride influx)

Diazepam is an anxiolytic that may also be used as a spasmolytic: exerts both antispasmodic and antispasticity actions

C/U: Oral formulation used in Cerebral palsy, multiple sclerosis, temporary muscle spasms (of any origin)

Management of anxiety disorders, symptomatic relief of agitation, tremor, and acute delirium in alcohol withdrawal

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8
Q

Gabapentin

Class and MOA, C/U?

A

GABA Agonist

Mechanism of Action:
INHIBITION of voltage-dependent calcium channels

An analog of GABA, but does not directly impact GABA receptor

Clinical Use:
Generalized tonic-clonic seizures
Neuropathic pain and post herpetic neuralgia pain
Diabetic neuropathy (off-label)

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9
Q

Pregabalin

CLASS AND MOA, C/U ?

A

GABA Agonist

Mechanism of Action:
Inhibition of voltage-dependent calcium channels.

GABA derivative similar to gabapentin

Clinical Use:
Partial-onset seizure (adjunct)
Non-epileptic: neuropathic pain associated with diabetic neuropathy, restless leg syndrome, post-herpetic neuralgia, fibromyalgia, pain due to spinal cord injury, social phobia

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10
Q

Botulinim Toxin A

Class and MOA, C/U ?

A

Direct/peripherally acting MSK relxant

Mechanism of Action:
Inhibits the release of acetylcholine from cholinergic nerve fibers at neuromuscular junctions

Produced by the bacteria clostridium botulinum

Botulism is a rare but serious paralytic illness

Poisoned victim becomes gradually weaker as nerves lose their ability to stimulate muscle contraction

C/U: (Toxin A only)

headache ≥15 d/mo x 3 mo;
≥8 headaches/mo
or migraines w/o aura

ALso, Cervical dystonia and blepharospasm

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11
Q

Dantrolene Sodium

Class and MOA, C/U?

A

Direct/peripherally acting MSK relxant

Mechanism of Action: reduces skeletal muscle strength by interfering with excitation-contraction coupling in the muscle fibers

C/U:
IV: Drug of choice in the treatment of malignant hyperthermia (MH)

ORAL: Chronic spasticity resulting from upper motor neuron disorders (eg. Spinal cord injury, stroke, cerebral palsy, or MS)

Not indicated for skeletal muscle spasm resulting from rheumatic disorders (i.e., Chorea, Rheumatic Fever)

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12
Q

Dicyclomine

Class, MOA, and Clin Use

A

Antispasmodic Agent MSK relax

Antispasmodic Agents: Used in treatment of smooth muscle disorders (ie. irritable bowel syndrome)
All Centrally and Peripherally acting

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13
Q

Hyoscyamine

Class, MOA, C/U

A

Antispasmodic Agent MSK relax

Antispasmodic Agents: Used in treatment of smooth muscle disorders (ie. irritable bowel syndrome)
All Centrally and Peripherally acting

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14
Q

Succinylcholine

A

Short Acting NMB

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15
Q

Atracurium

A

Intermediate Acting NMB
(non depol)

Metz to laudanosine

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16
Q

Cisatracurium

A

Intermediate NMB

NONdepol

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17
Q

Rocuronium

A

Intermediate NMB

NONdepol

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18
Q

Vecuronium

A

Intermediate NMB

NONdepol

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19
Q

Pancuronium

A

Long acting Non Depol NMB

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20
Q

What is the MOA of antispastic agents

A

reduce muscle cramping and tightness in neurological disorders and spinal cord injury and disease

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21
Q

Methocarbamol

Class and MOA

A

CNS depressant MSK relaxant antispamodic

MOA: unknown; suppresses spinal polysynaptic reflexes

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22
Q

Butalbital in Fioricent and Fiorinal

Class, MOA, C/U

A

Acetaminophen combinations

MOA: short- to intermediate-acting barbiturate

Can be used to Tx migraines however, No randomized, placebo-controlled studies support the efficacy of butalbital containing products in treating migraine headaches

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23
Q

Midrin C-IV

Class, MOA, C/U

A

Combination drug of acetaminophen 325 mg, isometheptene 65 mg, dichloralphenazone 100 mg

Mechanism of Action:
-Acetaminophen: analgesic

-Isometheptene: sympathomimetic amine that produces vasoconstriction of arteries and veins

-Dichloralphenazone: 1:2 phenazone: chloral hydrate mixture
—Phenazone: analgesic
—Chloral hydrate: sedative/hypnotic

Clinical Use:
Alternative choice for patients with mild-to-moderate migraine headache attacks

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24
Q

Excedrin OTC

CLASS, MOA, C/U

A

Combination drug: acetaminophen 250 mg, aspirin 250 mg, caffeine 65 mg

Clinical Use: reasonable first-line treatment choice for mild-to-moderate migraine attacks or severe attacks that have been previously responsive

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25
What is the MOA of ergotamine
Mechanism of Action: partial agonist activity at 5HT and D2 and alpha-adrenergic receptors C/U: migraine relief Caffeine: potentiates and increases ergotamine’s vasoconstrictive properties and absorption
26
What is the MOA and clin use of Digydroergotamine
Mechanism of Action: similar to ergotamine, with less potent α1-adrenergic vasoconstriction C/U: D.H.E. 45: IV IV used in the treatment of status migrainosus (Raskin protocol) D.H.E. subQ/IM/IV/nasal is a reasonable choice when the headache is moderate-to-severe or an adequate trial of NSAIDs or other non-opiate analgesics (including combo’s) have failed to provide adequate relief in the past* D.H.E. IV plus anti-emetics IV is an appropriate treatment for patients with severe migraine
27
What is the MOA and C/U of triptans
Mechanism of Action: 5-HT1B/1D receptor agonists with additional activity at 5HT1F receptors -5-HT1B cranial vasoconstriction -5-HT1D peripheral neuronal inhibition (e.g., CGRP, substance P, etc.) -5-HT1B/1D/1F inhibition of the trigeminocervical complex (i.e., decreased excitability) Clinical Use: appropriate 1st line therapy for patients with moderate to severe migraine and are used for rescue therapy when nonspecific medications are ineffective
28
What is the MOA and C/U of Cyproheptadine
Tx of Seretonin Syndrome 1st generation antihistamine, and 5HT1A and 5HT2 antagonist
29
Sumatriptan/ Naproxen MOA and C/U
Mechanism of Action: designed to target different vascular and inflammatory processes in a migraine Clinical Considerations: combination provides superior relief to either component
30
Butorphanol | MOA and C/U
Mechanism of Action: - Partial agonist - Partial mμ and kappa receptor agonist Formulations: IV, nasal spray Clinical Use: - Pain management - Pain during labor (if epidural is not possible) - Off label: Migraine (as last resort)
31
Metoclopraminde | MOA and C/U
Antiemetic | Use for the Tx of N/V assoc. with migraine Considered the best option
32
Chlorpromazine | MOA and C/U in migrianes
Typical Antipsychotic (1st Generation): dopamine and serotonin antagonist Used an an antiemetic in migraine Tx
33
Prochlorperazine | MOA and C/U for Migraines
Typical Antipsychotic (1st Generation): dopamine and serotonin antagonist Used as an antiemetic in Migraine Tx
34
Ondansetron | MOA and C/U with migraines
Seretonin antagonist Antiemetic
35
Granisetron | MOA and C/U in migraines
5HT3 antagonist Antiemetic
36
What is the MOA of CGRP Inhibitors
Inhibit Activation of trigeminovascular system results in decreased CGRP circulation Reducing migraine and light sensitivity
37
Erenumab-aooe | Class and C/U
CGRP antagonists Migraine prophylaxis in adults
38
Fremanezumab-vfrm | Class and C/U
CGRP antagonist Migraine prophylaxis in adults
39
Galcanezumab-gnlm | Class and C/U
CGRP antagonists Migraine prophylaxis in adults Tx od episodic cluster HA
40
Amitryptyline | Class, and C/U in tension HA
TCA DOC for Prophylaxis Tension HA
41
Verapamil | Class and C/U in HA
CCB Considered the drug of choice in Maintenance Prophylaxis (Effective in ~ 70% of patient)
42
Prednisone | C/U in HA
Prophylactic Tx of Cluster HA
43
Insulin | MOA
Mechanism of Action: Replaces (T1DM) or supplements (T2DM) endogenous insulin Facilitates glucose uptake into insulin-sensitive peripheral tissues Inhibits hepatic glucose output and glucagon secretion Ultimately reduces glucose in circulation
44
Insulin Lispro | Drug class
Rapid acting insulin
45
Insulin Aspart | Drugg class
Rapid acting insulin
46
Insulin Glulisine | Drugg class
Rapid acting insulin
47
Afrenza | Drug class
Inhaled insulin
48
Humulin R Drug class
Short acting Insulin
49
U-500 insulin C/U
Highly concentrated form of human regular insulin (i.e., 500 units/ml vs normal 100 units/ml) Used in patients with severe insulin resistance (i.e., require insulin doses > 200 units/day)
50
NPH (humulin N) Drug class
Intermediate acting insulin
51
NPH (Novolin N) Drug class
Intermediate acting insulin
52
Insulin glargine Drug class
Long acting insulin
53
Insulin Detemir Drug class
Long acting insulin
54
What is the MOA and C/U of Biguanides
Decreases hepatic glucose production (gluconeogenesis), glycogenolysis, and enhances insulin sensitivity in fat and peripheral (muscle) tissues (improves glucose uptake and utilization) Slows intestinal absorption of sugars Allows for an increased uptake of glucose into insulin-sensitive tissues C/U: 1st line for T2DM -Demonstrated improved cardiovascular outcomes Polycystic ovary syndrome (PCOS)
55
Metfromin | Drug class
Biguanide
56
What is the MOA and C/U of Sulfonylreas
Mechanism of Action: binds to a specific sulfonylurea receptor (SUR) on the pancreatic β cell leading to stimulation of insulin secretion (2nd phase) C/U T2DM
57
Chlorpropamide Drug class
1st gen Sulfonylureas
58
Tolazamide Drug class
1st gen sulfonylurea
59
Tolbutamide | Drug class
1st gen Sulfonylurea
60
Glipizide Drug class
2nd gen sulfonylurea
61
Glyburide Drug class
2nd gen. sulfonylurea
62
Glimepiride Drug Class
2nd gen sulfonylurea
63
What is the MOA and C/U of meglitinides
Stimulate insulin secretion from the β-cells of the pancreas, similarly to sulfonylureas (but different site) Require the presence of glucose to stimulate insulin secretion C/U; 2nd or 3rd line T2DM
64
Nateglinide Drug class
Meglitidines
65
Repaglinide Drug class
Meglitidines
66
What is the MOA and C/U of thiazolidinediones (TZDs)
Mechanism of action: Enhances insulin sensitivity in muscle and fat by increasing glucose transporter expression Binds the peroxisome proliferator activator receptor-γ (PPAR-γ) enhancing insulin sensitivity at skeletal muscle, liver, and fat cell Pioglitazone is also a partial agonist at PPAR-α (similar to fibric acid derivatives) Clinical Use: T2DM
67
Pioglitazone Drug class
TZDs
68
Rosiglitazone Drug class
TZD
69
What is the MOA and C/U of DPP-4 Inh
Mechanism of Action: Inhibits the enzyme DPP4, which prevents the degradation of endogenous incretins (GLP-1 and GIP) which increases insulin secretion, decreases glucagon secretion (glucose-dependent) No effect on gastric emptying and satiety Orally active Clinical Use: T2DM
70
Sitaglipin Drug class
DPP-4 inhb
71
Saxagliptin Drug class
DPP-4 inhb
72
Linagliptin Drug class
DPP-4 inhb
73
Alogliptin Drug class
DPP-4 inhb
74
What is the MOA and Clin use of GLP-1 agonists
Mechanism of Action: Stimulates GLP-1 receptors which increases production of insulin secretion in response to high blood glucose levels Suppresses postprandial glucagon secretion Slows gastric emptying Reduces food intake (i.e., increases satiety) Stimulates β-cell proliferation, preservation, and function in animals Clinical Use: T2DM
75
Exanatide Drug class
GLP-1
76
Liraglutide Drug class
GLP-1
77
Semaglutide Drug class
GLP-1
78
Dulaglutide Drug class
GLP-1
79
What is the MOA and C/U of Sythentic Amylin Analogues
Mechanism of Action: Suppress inappropriate high postprandial glucagon secretion Increases satiety (may result in weight loss) Slows gastric emptying: improves the rate of glucose appearance in the plasma Clinical Use: adjunct to mealtime insulin therapy in T1DM and T2DM
80
Pramlintide Drug class
Synthetic amylin analogue
81
What is the MOA and clin use of Alpha glucosidase inhibitors
Mechanism of Action: Competitively inhibit α-glucosidase enzymes (maltase, isomaltase, sucrose, and glucoamylase) in the small intestine delaying the breakdown of sucrose and complex carbohydrates to glucose and other monosaccharides Net effect is a reduction in the post-prandial blood glucose Absorption of glucose, lactose, and fructose not affected Clinical Use: T2DM -Good for patients near target HbA1c levels with near normal FPG levels, but high postprandial levels
82
Acarbose Drug Class
Alpha glucosidase inhibitors
83
Miglitol Drug class
Alpha glucosidase inhibitors
84
What is the MOA and C/U of SGLT2s
MOA: Inhibits the sodium glucose co-transporter 2 (SGLT2) transporter, which reduces reabsorption of filtered glucose and lowers the renal threshold for glucose, resulting in increased urinary glucose excretion C/U: T2DM Empagliflozin and Canagliflozin FDA approved for reducing CV events
85
Canagliflozin Drug class
SGLT2
86
Dapagliflozin Drug class
SGLT2
87
Empagliflozin Drug class
SGLT2
88
What is Corticorelin Ovine Triflutate
Synth CRH used to Dx between pituitary (Cushing’s Disease) and ectopic production of adrenocorticotropic hormone (ACTH)
89
What is the MOA and C/u of GNRH and LHRH
MOA: Sustained non-pulsatile administration results in suppression of ovarian and testicular steriodogensis due to decreased levels of LH and FSH Pulsatile administration is required to stimulate the gonadotroph cell to produce and release LH and FSH C/U : Treat infertily inhibit gonadal function in children with precocious puberty CAn be used for transgenderes to block puberty Tx of prostate cancer in men ART in women Ovarian supprsion in gyno d/.o
90
What is Gonadorelin
Gonadotropin Releasing Hormone (GnRH) Luteinizing Hormone-Releasing Hormone (LHRH) Agents
91
What is goderelin
Gonadotropin Releasing Hormone (GnRH) Luteinizing Hormone-Releasing Hormone (LHRH) Agents
92
What is Leuprolide
Gonadotropin Releasing Hormone (GnRH) Luteinizing Hormone-Releasing Hormone (LHRH) Agents
93
What is Nafarelin
Gonadotropin Releasing Hormone (GnRH) Luteinizing Hormone-Releasing Hormone (LHRH) Agents
94
What is histrelin
Gonadotropin Releasing Hormone (GnRH) Luteinizing Hormone-Releasing Hormone (LHRH) Agents
95
What is triptorelin
Gonadotropin Releasing Hormone (GnRH) Luteinizing Hormone-Releasing Hormone (LHRH) Agents
96
What is the class and C/u of Ganirelix
GnRH Receptor Antagonists Agent Inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation procedures
97
What is the class and C/u of Cetrorelix
GnRH Receptor Antagonists Agent Inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation procedures
98
What is the class and C/u of degarelix
GnRH receptor antagonist For men with advanced prostate cancer (dega is for the dicks)
99
MOA and C/u of GHIH
Bind to pituitary somatostatin receptors and block growth hormone (GH) secretion Also inhibits insulin, glucagon and gastrin secretion Clinical Use: Used to reduce symptoms caused by a variety of hormone-secreting tumors —Acromegaly and control symptoms of secretory diarrhea caused by vasoactive intestinal peptide (VIP) [VIP-secreting tumors] —Useful for the acute control of bleeding from esophageal varices (IV octreotide)
100
What is the class and C/u for octreotide
GHIH, used for esophageal varicies
101
What is the MOA and C/u of lanreotide
GHIH and used for acromegaly only
102
MOA and C/u of Pegvisomant
Mechanism of Action: Binds to growth hormone receptors on cell surfaces, where it blocks the binding of endogenous GH, thus interfering with GH signaling pathways Decrease IGF-1 concentrations Clinical Use: Treatment of acromegaly resistant to or unable to tolerate other therapies
103
What is thyrotropin alfa MOA and C/u
TSH Clinical Use: diagnostic agent for detecting blood levels of thyroglobulin to exclude the diagnosis of residual or recurrent thyroid cancer following a thyroidectomy
104
What is the Class and C/u of Follitropin alpha and beta | Also Urofollitropin and Lutropin alfa
FSH/LH ``` Clinical Use: Ovulation induction (FSH) ``` Ovulation induction (LH) in infertile females with LH deficiency Male Infertility (Spermatogenesis induction) (FSH)
105
MOA and C/u of Dopamine Agonists
MOA: Effectively suppress prolactin release, shrinks pituitary prolactin-secreting tumors, lower circulating prolactin levels, and restore ovulation in 70% of women with microadenomas and 30% of women with Adenomas Adenomas that secrete excess prolactin usually retain the sensitivity to inhibition by dopamine exhibited by the normal pituitary Clinical Use: Treatment of hyperprolactinemia Treatment of prolactin-secreting adenoma Treatment of acromegaly (monotherapy or in combo with pituitary surgery, radiation, and/or octreotide administration)
106
What is the class of bromocriptine
Dopamine agonist
107
Class of Cabergoline
Dopamine agonist
108
MOA and Clin/use of Conivaptan
Vasopressin antagonist SIADH
109
MOA and C/U of Tolvaptan
Vasopression antagonist SIADH
110
What is the Clin use of Pitocin
Labor stimulation and post partum bleeding
111
What is the MOA and C/U of Methimazole
Mechanism of action: Inhibits thyroid peroxidase, thus blocking iodination and synthesis of thyroid hormones Preferred agent for Grave’s diseases for most patients unless in 1st trimester of pregnancy (PTU preferred in this case)
112
What is the MOA and C/U of Propythiouracil
Mechanism of action: Inhibits thyroid peroxidase, thus blocking iodination and synthesis of thyroid hormones PTU may block T4 to T3 conversion in the peripheral as well Used during the 1st trimester of pregnancy, thyroid storm, and in those experiencing adverse reactions to methimazole (other than agranulocytosis or hepatitis)
113
What is the MOA and C/U of Iodides
Mechanism of action: Acutely inhibits hormonal secretion within hours Temporary inhibition of thyroid hormone synthesis Reduces the thyroid gland’s vascularity (thereby increasing firmness) and decrease size prior to thyroidectomy C/U Short term preop or before rads

IPAP JUNIOR SEM. (43 decks)

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