Uterine, Thyroid, & Osteoporosis Drugs Flashcards

(61 cards)

1
Q

Oxytocin (Pitocin®, Syntocin®) - Indications/Therapeutics

A

• DOC to induce labor at term if indicated
– Augment labor in selected patients with uterine dysfunctional inertia
– Causes timed contractions (on then off)
– IV infusion is preferred for these
• For prevention of hemorrhage
– IM route is preferred for this
• For stimulation of milk let-down reflex
– Nasal application method (Cotton pledget)

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2
Q

Oxytocin (Pitocin®, Syntocin®) - Adverse Effects

A

• Water intoxication with convulsions
– Because of ADH like effect of oxytocin
– Serious complication that may occur
– If doses are large and infused for a prolonged period
• Uterine rupture with large dose
• Allergy
• Anaphylaxis
• Sinus bradycardiaof the fetus
– Premature ventricular contractions and other
arrhythmias of the fetus and fetal death due to
extreme uterine contractions, etc.

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3
Q

Oxytocin (Pitocin®, Syntocin®) - Pharmacokinetics

A
  • Very short half-life: 1-6 minutes

* Inactivated by liver and kidneys

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4
Q

Oxytocin (Pitocin®, Syntocin®) - Contrindications/Precautions

A
  • Malpresentation
  • Cephalopelvic disproportion
  • Complete placenta previa
  • Uterine scar from previous cesarean section
  • Unengaged head
  • Cervical scarring
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5
Q

Ergonovine maleate (Ergotrate®) - MoA

A

• Contraction of uterine smooth muscle through

activation of serotonin and a-adrenergic receptors

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6
Q

Ergonovine maleate (Ergotrate®) - Indications/Therapeutics

A

• After completion of labor and the delivery of the
placenta to produce firm uterine contractions and to
decrease uterine bleeding
– 2nd line after massage and oxytocin have failed
• For the same reasons following suction abortion

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7
Q

Ergonovine maleate (Ergotrate®) - Pharmacokinetics

A

• Rapid action
– 30-40 seconds after IV
– 10 minutes after oral use
• Action lasts several hours

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8
Q

Ergonovine maleate (Ergotrate®) - Adverse Effects

A
  • Transient hypertension – Contracts all smooth muscle

* Angina, MI

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9
Q

Ergonovine maleate (Ergotrate®) - Contraindications/Precautions

A

• C/I: Should never be used to induce labor.
– The contractions are strong, non-physiological,
continuous and will cause fetal hypoxia.
• Peripheral vascular or coronary artery disease

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10
Q

Prostaglandins

A

Dinoprostone (ProstinE2®)
Carboprost tromethamine (Prostin/M15®, Hemabate®)
Misoprostol (Cytotec®)

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11
Q

Prostaglandins - Indications/Therapeutics

A

• Expulsion of uterine contents (all):
– Intrauterine fetal death
– Missed abortion (miscarriage)
– Elective abortion
• Cervical ripening prior to delivery at term
(dinoprostone only)
• Postpartum bleeding due to uterine atony
– 3rd line, after massage, oxytocin, and ergots

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12
Q

Prostaglandins - Pharmacokinetics

A
  • For abortion & PPH: vaginal or rectal suppositories/pill
  • For cervical ripening: apply gel to cervix
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13
Q

Prostaglandins - Adverse Effects

A
  • G.I. disturbances, vomiting, diarrhea -Black Box
  • 30-70% experience fever, chills, headache
  • Many common but not serious (use correct dose)
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14
Q

Prostaglandins - Contraindications/Precautions

A

• For cervical ripening, problems with mother or fetus:
– Fetal distress, etc.
– History of difficult deliveries or caesarean section
• For abortions, should not be used in patients with:
– Acute pelvic inflammation
– C/I: Acute cardiac, pulmonary, renal, or hepatic
diseases
– Asthma, hypertension, anemia, jaundice or epilepsy

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15
Q

Tranexamic acid (Cyklokapron®) - Indications/Therapeutics

A

• Reduced death due to bleeding in women with
postpartum hemorrhage by 20-30% in trial
• Uterine bleeding (fibroids, other causes), when
hormonal therapy not wanted or C/I

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16
Q

Tranexamic acid (Cyklokapron®) - Pharmacokinetics

A

•Given IV
– Along with standard uterotonic therapy (should not
be regarded as an alternative therapy)

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17
Q

Tranexamic acid (Cyklokapron®) - Adverse Effects

A

• Can cause intravascular thrombosis

– Not seen in trial

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18
Q

Magnesium Sulfate (MgSO4) - MoA

A

• Relaxes the uterus probably by a direct effect

– Mechanism unknown

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19
Q

Magnesium Sulfate (MgSO4) - Indications/Therapeutics

A

• Considered 1st line drug
• Can prevent convulsions in pre-eclampsia and treat
eclampsia (FDA approved)

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20
Q

Magnesium Sulfate (MgSO4) - Pharmacokinetics

A

• IV, administered slowly (significant hypotension or

asystole if too fast)

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21
Q

Magnesium Sulfate (MgSO4) - Adverse Effects

A

• Flushing, diaphoresis, hypotension
• Depressed deep tendon reflexes, muscle paralysis,
weakness, lethargy, hypothermia
• Circulatory collapse, and cardiac, CNS, or respiratory
depression

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22
Q

Nifedipine (Procardia®)

A

• L-type calcium channel blocker

Mechanism of Action:
• Inhibits Ca2+influx (smooth muscle contractions)

Indications/Therapeutic Effects:
• Becoming 1st line agent (considering b2-agonists
problem)

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23
Q

Indomethacin (Indocin®) - MoA

A

• Inhibits COX enzyme: Reduction of prostaglandin

synthesis

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24
Q

Indomethacin (Indocin®) - Adverse Effects

A

• Maternal GI irritation, peptic ulceration,
thrombocytopenia, allergic reactions, headaches and
dizziness
• There are reports about partial closure of the fetal
ductus arteriosus, impaired fetal renal function,
bronchopulmonary dysplasia and persistent pulmonary
hypertension in the neonatal period

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25
Progesterone - Indications/Therapeutics
• More effective than placebo in maintaining the length of pregnancy when given prophylactically from the 16th - 37th week of pregnancy or until delivery – Not effective for acute treatment • Recommended for high risk women with a history of preterm birth • Approved for use in ART to maintain the luteal phase following IVF or ICSI.
26
Levothyroxine sodium (Synthroid®)
• T4, produces normal levels of T3 and T4 • Drug of choice for hypothyroidism • Drug levels must be carefully titrated to the individual – TSH levels & Patient Sx • T4 levels change slowly (t½= 7 days), ~5 weeks for steady state
27
Liothyronine sodium (Cytomel®)
• T3; t½= 24 hrs, shorter duration of action than T4 • Used for initial therapy (quicker steady state), not maintenance
28
Dessicated Thyroid (Armour Thyroid®)
• Mix of T4 and T3 hormones from pigs -> natural hormones • Batch potency can vary • Pts w/ deficiency in the peripheral deiodinase enzyme may respond better to this drug.
29
Thioamides
Propylthiouracil (PTU) and Methimazole (Tapazole®)
30
Thioamides - MoA
``` • Inhibits the synthesis T4 – Methimazole more potent • PTU -> blocks conversion of T4 to T3 • Effects are gradual (use b-blockers) – Circulating T3/T4 lasts a week or so ```
31
Thioamides - Indications/Precautions
• First line of treatment for Graves’ – Medical management • Used with other treatments -> ↓thyroid storm risk
32
Thioamides - Adverse Effects
• Black Box Warning for PTU – Severe liver injury, acute liver failure – Methimazole DOC in most cases • Methimazole allergies and pregnancy -> PTU • Itching and skin rash –most common • Granulocytopenia and agranulocytosis – Reversible – Watch for sore throat, do blood test • Headaches, nausea, jaundice, myalgia, arthralgia, lymphadenopathy, psychosis, lupus-like syndrome • Goiter - may need to add T4 to reduce TSH levels • Keep dose low in pregnancy - Prevent cretinism and goiter in fetus
33
Iodide - MoA
• Iodide rapidly decreases synthesis and release of T4/T3 • Short-term effect (2-8 weeks)
34
Iodide - Indications/Therapeutics
• Decreases vascularity and thyroid content of gland • Used for 7-10 days before surgery – Can decrease likelihood of thyroid storm • Can use in radioactive emergencies
35
Radioactive Iodine – 131 I - MoA
• 131I taken into the gland specifically – Small amounts μCi = diagnostic – Large amounts mCi = destroys gland
36
Radioactive Iodine – 131 I - Indications/Therapeutics
• Used in elderly patients and those with heart disease – Definitive treatment for Graves’, but thioamides preferred • Preferred treatment for toxic nodular goiter -> specific destruction -> euthyroid
37
Radioactive Iodine – 131 I - Adverse Effects
• Usually causes hypothyroidism over time • Thyroid storm risk – Decrease risk by use of thioamide (not iodide!) prior to treatment
38
Radioactive Iodine – 131 I - Contraindications
• Pregnancy, nursing, or mothers who lack childcare
39
Beta-Blockers - MoA
• Non-specific β-blocker • Propranolol specifically inhibits the peripheral conversion of T4 to T3
40
Beta-Blockers - Indications/Therapeutics
• ↓many of the Sx of hyperthyroidism • Used to prepare for surgery and while waiting for thioamides or 131I to take effect
41
Beta-Blockers - Contraindications
• C/I: Asthma – use CCBs instead
42
Calcitonin (Miacalcin®) - MoA
* ↓ Bone resorption of Ca2+ * Antagonizes parathyroid hormone * ↓ Bone pain and loss * ↑ Bone density * ↓ Osteoporotic fractures
43
Calcitonin (Miacalcin®) - Pharmacokinetics
* Nasal spray | * Injection
44
Calcitonin (Miacalcin®) - Indications
* Osteoporosis – (not 1st line) | * Paget’s disease
45
Calcitonin (Miacalcin®) - Adverse Effects
* May cause allergic reactions * Nasal rhinitis/ sinusitis -> nasal spray * Nausea and vomiting -> injection
46
Parathyroid Hormone Drugs
Teriparatide (Forteo®) Abaloparatide (TYMLOS®) rhPTH(1-84) (NATPARA®)
47
Parathyroid Hormone Drugs - MoA
• PTH and PTHrP both bind to the PTH Receptor type 1 (PTHR1) on the osteoblast and activate it. • There are two conformations of PTHR1, RG and R0, which are pro-osteoblast or pro-osteoclast, respectively. Teriparatide -or- Abaloparatide: More osteoblast activity -> Osteoporosis rhPTH(1-84): More osteoclast activity -> Hypoparathyroidism
48
Teriparatide & Abaloparatide - Pharmacokinetics
• Subcutaneous injection – Teriparatide: peaks in 30 min, gone in 3 hours -> Intermittent
49
Teriparatide & Abaloparatide - Adverse Effects
* Hypercalcemia and hypercalciuria * Injection site reactions * Dizziness, leg cramps * Abaloparatide: hyperuricemia
50
Teriparatide & Abaloparatide - Contraindications
• Osteosarcoma (Black Label Warning) – ↑ in rats, but not in humans yet – Be careful in patients susceptible to any osteosarcoma (Paget’s disease, radiation therapy, open epiphyses, history)
51
Denosumab (Prolia®) - MoA
• Antibody against receptor activator of nuclear factor kappa-beta ligand (RANKL) • Inhibits bone resorption • Antibody to RANK-Ligand -> inhibits RANKL – Factor made by osteoblasts that is necessary for the formation of mature osteoclasts
52
Denosumab (Prolia®) - Indications/Therapeutics
• Osteoporosis in men and postmenopausal women at high risk for fractures • ↑ Bone mass and strength in both cortical and trabecular bone
53
Denosumab (Prolia®) - Pharmacokinetics
• S.C. injection, once/6 months
54
Denosumab (Prolia®) - Adverse Effects
* Hypocalcemia(2%) | * Osteonecrosis of the jaw in cancer studies
55
Denosumab (Prolia®) - Contraindications/Precautions
``` •Absolute C/I: – Hypocalcemia, fix first – Pregnancy – Cat X • Relative – Chronic Kidney Disease – Patients at risk for serious infections (RANK-RANKL signaling in lymphocytes ```
56
Bisphosphonates
Alendronate (Fosamax) - Oral Risedronate (Actonel) - Oral Ibandronate (Boniva) - Oral, I.V. Zoledronic Acid (Zometa) - I.V.
57
Bisphosphonates - MoA
``` • P-C-P bond analogs of pyrophosphate • Substitutes for PO4 in Ca2+ binding – Incorporates into bone • Inhibits osteoclast activity and bone resorption – Mechanism still not clear ```
58
Bisphosphonates - Indications/Therapeutics
``` • First line of treatment (DOC) for post-menopausal osteoporosis • Paget’s Disease • Osteopenia -> may not be needed • Reduce the incidence of fractures • Improve the quality of life ```
59
Bisphosphonates - Pharmacokinetics
• ORAL preparations: absorption is very poor – Must be taken on an empty stomach! – 1/2 glass of water – Stay upright for 30 min after taking it to decrease esophageal irritation • Others are IV injection only • Given anywhere from once/day to once/year
60
Bisphosphonates - Adverse Effects
• Oral -> abdominal pain, upper GI irritation, esophageal ulceration, constipation, diarrhea, and flatulence • I.V. -> renal toxicity if given too fast • Nausea, vomiting • May cause a mild hypocalcemia • Possible atrial fibrillation • ↑ Incidence of osteonecrosis of the jaw after major dental work • 2010 FDA safety communication: atypical bone fractures of the femur with long-term bisphosphonate therapy
61
Bisphosphonates - Contraindications/Precautions
• Oral: inability to stand/sit upright or esophageal disease • IV: renal disease