-
Acetylcholine
- •Category: ANS- Parasympathomimetic
- •MOA: Muscarinic and nicotinic agonist
- •Distinguishing characteristics:
- –Rapidly hydrolyzed by esterases
- –Acts on both muscarinic and nicotinic receptors
- –Quaternary ammonium group invokes polarity
- •Predictable characteristics:
- –Short half life (seconds)
- –Diffuse activity (parasympathomimetic, sympathomimetic and skeletal muscle)
- –Limited distribution
- •Predictable uses: Possible local ophthalmic use, but other products better.
-
Bethanechol
(URECHOLINE)
- •Category: ANS- Parasympathomimetic
- •MOA: Muscarinic agonist
- •Distinguishing characteristics
- –Not metabolized by esterase enzymes
- –Quaternary ammonium compound
- –Particular affinity for gut and bladder smooth muscle
- –Oral route preferred
- •Predictable characteristics
- –No CNS effect
- –T1/2 allows distribution to areas of low blood flow
- •Predictable uses
- –Gastroparesis (postoperative)
- –Urinary retention
- –Xerostomia
- –Ocular diagnostics
- •Predicable side effects
- –Other parasympathomimetic effects especially following parenteral Rx
-
Pilocarpine
- •Category: ANS- Parasympathomimetic
- •MOA: Muscarinic receptor agonist
- •Distinguishing characteristics
- –Plant origin- Pilocarpus jabarundi
- –Tertiary ammonium compound
- –Preferential activity on sweat glands
- –Resistant to esterases
- •Predictable characteristics
- –Used as miotic and in treatment of glaucoma
- –Will cause accommodation
- –Used to treat xerostomia
- –May cause CNS effects at high plasma levels
- –Diaphoresis is common side effect
- –Duration of action up to 8 hours
-
Neostigmine
- •Category: ANS- Parasympathomimetic
- •MOA: Reversible cholinesterase inhibitor
- •Distinctive characteristics:
- –Quaternary ammonium compound (contrast to physostigmine)
- –Contains ester group- slowly hydrolyzed (1-2 hr T1/2)
- –Poorly absorbed following oral Rx
- •Predictable activities
- –Elevates Ach levels
- –Causes both muscarinic and nicotinic stimulation
- –Numerous peripheral side effects but not CNS
- •Predictable uses
- –Miosis and Rx glaucoma (local administration)
- –Rx myasthenia gravis
- –Antidote to some drugs (atropine)
- –Atonic gut and bladder
-
Malathione
- •Category: ANS- Parasympathomimetic
- •MOA: Irreversible cholinesterase inhibitor
- •Distinguishing characteristics:
- –Tertiary ammonium compound
- –Binds covalently to esterase enzymes
- –Not hydrolyzed by esterase enzymes
- –Rapidly absorbed through multiple routes
- •Predictable characteristics
- –Causes SLUD and other ANS activities
- –Causes CNS disturbances
- –No therapeutic use
- –Used as insecticide
- –Similar agents used as chemical weapons
- –Atropine is antidote plus supportive therapy
-
Atropine
- •Category: ANS- Parasympatholytic
- •MOA: Muscarinic receptor antagonist
- •Distinguishing characteristics:
- –From plant source- Atropa belladona
- –Tertiary ammonium compound
- –Ester group required for activity
- –Resistant to hydrolysis by esterases
- –Metabolized in liver with T1/2 of about 4 hr.
- •Predictable activities:
- –CNS toxicity in especially in children even after ophthalmic Rx
- –Inhibit SLUD and other parasympathetic activities
- –Used in ophthalmology- mydriasis and cycloplegia
- –Used as antidote- parasympathomimetics
- –Used to treat diarrhea
- –Once used to treat asthma, but now better drugs available
-
Scopolamine
- •Category: ANS- parasympatholytic
- •MOA: Muscarinic receptor antagonist
- •Distinguishing characteristics:
- –From plant source- Hyocyamus niger
- –Greater CNS distribution than atropine
- –Other characteristics similar to atropine
- •Predictable actions:
- –Greater CNS side effects and abuse potential than atropine
- –Used less frequently than atropine
- –Used to treat motion sickness
-
Ipratropium(Atrovent)
- •Category: Parasympatholytic
- •MOA: Muscarinic antagonist
- •Distinguishing characteristics:
- –Quaternary ammonium compound
- –Minimal inhibition of mucociliary clearance
- •Predictable actions:
- –No CNS effects
- –Bronchodilation
- –Limited mucous accumulation
-
Muscarine
- •Category: ANS- Parasympathomimetic
- •MOA: Muscarinic receptor agonist
- •Distinguishing characteristics:
- –Naturally occurring
- –Quaternary ammonium compound
- –Found in Amanita muscaria, but not major toxic entity in mycetism
- •Predictable characteristics:
- –SLUD
- –No CNS activity
- –Greater historical than therapeutic importance
-
Epinephrine
- •Category: ANS- Sympathomimetic
- •MOA: Stimulate Alpha and Beta receptors (G protein which facilitate second messengers.)
- •Distinguishing characteristics:
- –Metabolized in gut, blood and multiple tissues
- –More Beta and less Alpha activity than norepinephrine
- •Predictable Characteristics & Uses
- –Ineffective orally
- –Very short half-life (minutes)
- –Cardiac emergencies
- –Brochospasm
- –Adjunct to local anesthesia
- •Predictable side effects
- –Tachycardia & increased force of contraction
- –Blood pressure disturbance (usually hypertension)
-
Phenylephrine(NEOSYNEPHRINE)
- •Category: ANS- Sympathomimetic
- •MOA: Alpha 1 receptor agonist
- •Distinguishing characteristics:
- –Effective orally
- –Limited access to CNS
- •Uses:
- –Nasal decongestant
- –Mydriatic
- •Side effects:
- –Rebound congestion
- –Increased peripheral resistance
- –Reflex bradycardia
-
Clonidine(Catapres)
- •MOA: Alpha 2 receptor agonist
- •Distinguishing characteristics
- –Effective orally
- –Crosses blood-brain barrier
- –Prefers alpha receptors in brainstem
- –Long half-life and duration of action
- –Diminish discharge from medular vasomotor center
- •Predictable uses: Antihypertensive
- •Predictable side effects:
- –Dry mouth
- –Sedation
- –Sexual dysfunction
-
Isoproterenol(ISUPREL)
- •Category: ANS- Sympathomimetic
- •MOA: Beta receptor agonist (Both 1 & 2)
- •Distinguishing characteristics
- –Metabolized by COMT
- –Short duration of action
- –Both beta 1 and beta 2
- •Predictable uses: Cardiac arrest
- •Predictable actions:
- –Tachycardia
- –Bronchodilation
- –Replaced often by more selective beta agonists (Why?)
-
ALBUTEROL(VENTOLIN
- •Category: ANS- Sympathomimetic
- •MOA: Beta 2 receptor agonist
- •Distinguishing characteristics
- –Effective orally or by inhalation
- –Limited cardiovascular effects
- –Duration of action several hours
- •Predictable uses: Bronchodilator
- •Predictable side effects:
- –Weak and occasional tachycardia
- –Vasodilation
-
Amphetamine
- •Category: ANS Sympathomimetic
- •MOA: Stimulate release of Norepinephrine and Dopamine
- •Distinguishing Characteristics:
- –Enters CNS
- –Inhibits MAO
- •Predicted actions:
- –Alpha and Beta Stimulation by norepinephrine: Vasoconstriction, cardiac stimulation, increased blood pressure, mydriasis
- –CNS stimulation: euphoria, insomnia, anxiety, loss of appetite, hyperthermia
- –Used to treat: narcolepsy, obesity and ADD
- –High abuse potential makes it scheduled substance
-
Substances that increase norepinephrine release:
- •Cocaine
- •Tyramine
- •Reserpine (although its overall effect is to deplete norepinephrine)
- •Ephedrine
- •Pseudoephedrin
- •Methamphetamine
-
Phenelzine(NARDIL)
- •Category: ANS- Sympathomimetic
- •MOA: Monoamine oxidase inhibitor
- •Distinctive characteristics
- –Readily absorbed
- –Crosses blood-brain barrier
- –Increases synaptic catecholamine levels
- •Predictable use: Antidepressant
- •Predictable side effects: Sympathomimetic actions
-
Prazocin(Minipress)
- •Category: ANS- Sympatholytic
- •MOA: Alpha 1 receptor antagonist
- •Distinctive characteristics:
- –Effective orally
- –Highly protein bound (5% free)
- –Limited reflex tachycardia
- •Predicted use: Hypertension
- •Predicted side effects:
- –Hypotension
- –Syncope
-
Propranolol(INDERAL)
- •Category: ANS- Sympatholytic
- •MOA: Beta 1 & 2 receptor antagonist
- •Distinguishing characteristics:
- –Very lipid soluble
- –Significant 1st pass metabolism
- –Highly variable plasma levels
- –Multiple uses (not all very predictable)
- •Uses
- –Antihypertensive
- –Antiangina
- –Antiarrythmic
- •Side effects
- –Place asthma patients at risk
- –Place diabetics at risk
-
Metoprolol(LOPRESSOR)
- •Category: ANS- Sympatholytic
- •MOA: Beta 1 receptor antagonist
- •Distinctive characteristics:
- –Similar to propranolol
- •Uses: Antihypertensive without risk to asthmatics and diabetics
-
Reserpine
- •Category: ANS- Sympatholytic
- •MOA: Promotes release of Norepinephrine and reduces reuptake resulting in depletion of norepinephrine stores
- •Distinctive characteristics:
- –Derived from plant
- –Transitory sympathomimetic followed by prolonged sympatholytic effect
- –Antiquated for therapeutic use, extensive research use
- •Predictable uses: Antihypertensive
- •Predictable side effects: Prolonged paralysis of sympathetic nervous system
-
Levodopa
- Category: Anti-parkinson
- Mechanism of Action: Replace dopamine, the neurotransmitter that is absent in Parkinson’s Disease
- Distinguishing Characteristics:
- Levodopa converted to dopamine in brain
- Dopamine destroyed in gut and doesn’t cross BBB.
- Dopamine is sympathomimetic
- Predictable actions:
- Sympathomimetic side effects
- Often given with carbidopa (a drug that prevents conversion of dopa to dopamine in periphery) to reduce sympathomimetic side effects.
-
Sertraline(Zoloft)
- Category: Antidepressant
- Mechanism of Action: Selective serotonin reuptake inhibition(SSRI)
- Distinguishing Characteristics:
- –Must “titrate” dose for optimum effect
- Predictable Actions:
- –Similar Action to other SSRIs:
- •Escitalopram (Lexapro)
- •Fluoxetine (Prozac)
- –Side effects related to serotonin activity (central & peripheral)
- •Insomnia
- •Headache
- •Nausea
- •Dry mouth
-
Venalfaxine(Effexor)
- Category: Antidepressant
- Mechanism of Action: Non-selective neurotransmitter reuptake inhibition
- Distinguishing Characteristics:
- –Increase levels of serotonin, norepinephrine and dopamine in central and peripheral synapses
- Predictable actions:
- –Side effects related to all of the neurotransmitters
- •Hypertension or hypotension
- •Tachycardia
- •Insomnia
- –Similar Drugs:
- •Trazadone (Desyrel)
- •Bupropion (Wellbutrin)
-
Monoamine inhibitors:
- –Increase amount of norepinephrine, dopamine and serotonin in synapse by decreasing metabolism
- –Includes: Tranylcypromine (Parnate)
- –Reacts with other sympathetic drugs
-
Phenytoin
- Category: Antiseizure
- MOA: Inhibit Na channels
- Unique Characteristics:
- –Hydantoin derivative (Formerly known as diphenylhydantoin)
- –Poor water solubility causes variable bioavailability
- –Metabolized by cytochrome p450 system (induces CYP3A4 isoenzyme)
- –Side effects:
- •Interferes with folate metabolism
- •Causes gingival hyperplasia
- •May cause hirsutism
- –Indications
- •Partial seizures
- •Generalized tonic-clonic seizures
- Predicted Actions
- –Accelerates metabolism of valproate, digoxin, steroids, vitamin K
- –Monitor plasma levels especially when changing formulations
- –Folate-related side effects and teratologies
-
Gabapentin
- Category: Antiseizure
- MOA: Increases release of GABA
- Unique Characteristics:
- –Short half-life
- –Few side effects
- –Indications: Adjunct to other antiseizure drugs
- Predictable Actions:
- –Rx several times daily
- –Rx broad spectrum of seizures
-
Two types of analgesics:
- –Narcotic (Morphine, hydrocodone, oxycodone, Pentazocine, Meperidine, propoxyphen)
- –Non-narcotic (Acetaminophen, aspirin, ibuprophen)
-
some combinations of analgesics
- –Hydrocodone + acetaminophen = Vicodin
- –Acetaminophen + codeine = Tylenol with codeineOxycodone + aspirin = Percodan
-
Analgesic mechanisms of action
- –Narcotics stimulate opiate receptor in thalamus
- –Non-narcotic block enzymes responsible for producing prostaglandins and other chemical transmitters
-
Hydrocodone
- Category: Analgesic
- Mechanism of Action: Opiate receptor agonist (especially in thalamus, brainstem, gut, eye)
- Distinguishing Characteristics:
- –Scheduled substance (2-3)
- –Tolerance upon repeated use
- Predictable Actions:
- –Pain less objectionable
- –Depresses respiratory center, overdose causes apnea
- –Physical and psychological dependance
- Similar drugs include oxycodone, morphine
-
Tramadol
- Category: Analgesic
- Mechanism of Action: Opiate receptor agonist in thalamus also inhibits reuptake of serotonin and norepinephrine
- Distinguishing characteristics:
- –May lower seizure threshold
-
Alprazolam(Xanax)
- Category: Anxiolytic, Sedative Hypnotic, Anti-epileptic, Muscle Relaxant
- Mechanism of Action: GABA receptor agonist (Gama-aminobutyric Acid is inhibitory neurotransmitter)
- Distinguishing Characteristics:
- –Benzodiazapine
- Similar drugs include: Lorazepam, Clonazepam, Diazepam (Differ in onset and duration of action)
-
Benzodiazapines
- •Diazepam (Valium) – Anxiety
- •Flurazepam (Dalmane) – Insomnia
- •Clonazepam (Klonopin) – Anxiety
- •Chlordiazepoxide ( Librium) – Anxiety
- •Lorazepam (Ativan) - Sedation
- •Oxazepam ( Serax) – Anxiety in hepatic pts.
-
PLF of Procaine (Novocaine)
- •Category: Local Anesthetic
- •MOA: Sodium Channel Inhibition
- •Distinguishing Characteristics:
- –Ester-linked
- –First synthetic local anesthetic
- –Diminished contemporary use
- •Predictable Qualities:
- –Quickly metabolized
- –Metabolized to PABA
- –High incidence of hypersensitivity
-
PLF of Lidocaine(Xylocaine)
- •Category: Local Anesthetic
- •MOA: Sodium Channel Inhibition
- •Distinguishing Characteristics:
- –Amide-linked local anesthetic.
- –Topical and parenteral preparations
- –Used as antiarrythmic
- •Predictable Qualities:
- –Most commonly used local anesthetic
- –Low incidence of hypersensitivity
- –Wide variance of applications
-
PLF of Benzocaine
- •Category: Local Anesthetic
- •MOA: Sodium Channel Inhibition
- •Distinguishing Characteristics:
- –Ester-linked
- –Low solubility
- –Used topically
- •Predictable Qualities
- –Sunburn Ointments
- –Over the counter
-
PLF of Cocaine
- •Category: Local Anesthetic and Sympathomimetic
- •MOA: Sodium Channel Inhibition
- •Distinguishing Characteristics:
- –Ester-linked
- –Sympathomimetic
- –Inhibits norepinephrine uptake
- –CNS stimulation (euphoria)
- •Predictable qualities
- –High abuse potential
- –Vasoconstrictor
- –Used in topical anesthesia of upper respiratory tract (mucosal vascular constriction)
-
Levothyroxine
- Category: Thyroid Drug
- MOA: Bind to nuclear receptors that cause gene transcription and protein synthesis
- Unique Characteristics:
- –T4
- –Converted to T3 (some in periphery, remainder in cell)
- –Half-life 7 days
- –80% bioavailability
- –Metabolized in cytochrome P450 system
- –Highly protein bound (99%+)
- Predictable Actions
- –Slow onset of action (Week or more)
- –Daily administration
- –Drug interactions due to metabolism and protein binding
- –Drug of choice for replacement and suppression therapy
-
Liothyronine
- Category: Thyroid Drug
- MOA: Bind to nuclear receptors that cause gene transcription and protein synthesis
- Unique Characteristics:
- –T3
- –95% bioavailable
- –Several times more potent than T4
- –Similar protein binding and metabolism to T4
- Predicted Actions:
- –Less physiologic than T4
- –Disturb thyroid function tests
-
Iodide Salts
- Category: Antithyroid
- MOA: Inhibit release of thyroid hormones
- Unique Characteristics:
- –Include potassium iodide
- –Rapid onset of therapeutic effect (2-7 days)
- –Often accompanied by propylthiouracil therapy
- –Metalic taste, hypersensitivity
- Predicted actions:
- –Treatment of thyroid storm with beta blockers
-
Propylthiouracil
- Category: Antithyroid Drug
- MOA: Inhibit several steps in thyroid hormone synthesis (peroxidase steps and coupling)
- Unique Characteristics:
- –Accumulate and stored in thyroid
- –Therapeutic effects must await exhaustion of stored hormones
- –Cross placenta
- Predictable Characteristics:
- –Pregnancey Category D
- –Long onset of therapeutic effect
-
Radioactive Iodine
- Category: Antithyroid
- MOA: Diagnostic and chemical ablation
- Unique Characteristics:
- –Iodine isotope 131
- –Rapidly absorbed
- –Concentrated and stored in gland
- –Emits beta rays with half-life of 5 days
- –Painless and few side effects
- –Cross placenta
- Predicted Activity
- –Destroy thyroid tissue
- –Contraindicated in pregnancy
-
Insulin
- Category: Antidiabetic
- MOA: Binds to insulin receptors activates tyrosine kinase phosphorylates proteins alter metabolic enzymes. MOVES GLUCOSE INTO CELL FROM PLASMA
- Unique Characteristics:
- –Protein
- –Short half-life (3-5 min)
- –Multiple forms differ in solubility and release from site of injection.
- Predictable actions:
- –Causes decreased plasma glucose
- –Treat type 1 diabetes and occasional type 2 diabetes
- –Ineffective orally (Rx subcutaneously, usually)
- –Repeated injections
- –Will cause hypoglycemia when in excess
-
Glucagon
- Category: Pancreatic Hormone
- MOA: Bind to receptors in liver cause increased cAMP and glycogenolysis and gluconeogenesis
- Unique Characteristics:
- Polypeptide (29 amino acids)
- Half-life 3 to 6 min.
- Predictable Actions:
- –Raise blood glucose at expense of stored hepatic glycogen.
- –Rx parenterally
- –Emergency treatment of severe hypoglycemia
- –Increased cAMP levels in heart may treat beta agonist toxicity
-
Estrogens
- Category: Estrogen
- MOA: Bind to estrogen receptors in nuclei of target cells to regulate protein synthesis.
- Unique Characteristics:
- –Absorption varies widely with salt and formulation.
- –Transdermal, oral, parenteral forms
- –Highly protein bound, compete with thyroid and other drugs.
- –Linked to breast cancer
- Predicted actions:
- –Hormone replacement therapy (postmenopausal)
- –Oral contraception
-
Progesterone
- Category: Progestin
- MOA: Bind to progesterone receptors in nuclei of target cells to regulate gene transcription in diverse cells.
- Unique Characteristics:
- –Rapidly absorbed following oral administration.
- –Metabolized in liver on first pass.
- Predictable Actions:
- –Hormone Replacement Therapy (menopause)
- –Contraception
-
Clomiphene
- Category: Antiestrogen
- MOA: Partial antagonist at estrogen receptor.
- Unique Characteristics:
- –Blocks estrogen receptors in anterior pituitary
- –Hot flashes similar to post-menopausal
- Predictable Effects:
- –Diminishes negative feedback inhibition
- –Allows increase in LH and FSH
- –Promotes ovulation
- –Incidence of multiple pregnancy is 10%
- –Used a fertility medication
-
Mifepristone
- Category: Antiprogesterone
- MOA: Competetive antagonist of progesterone.
- Unique Characteristics:
- –Also known as RU 486 or “morning after pill”
- –Prevents progesterone from maintaining endometrium for implantation
- –Also binds to glucocorticoid receptor
- Predicted actions:
- –Emerging value as antineoplastic agent
-
Oral Contraceptives
- Category: Oral Contraceptive
- MOA:
- •Selective inhibition of pituitary function resulting in anovulation
- •Change in cervical mucus
- •Change in endometrium
- •Uterine and fallopian tube motility
- Unique Characteristics:
- •Return to normal menstrual patterns following years of contraception
- •Breast enlargement and diminished lactation
- •Increase cortisol and cortisol binding proteins
- •Increase thyroxin and thyroxin binding proteins
- •Modifications in blood clotting
- •Increased plasma triglycerides
- •Increased risk of hypertension and myocardial infarct
- Predictable actions:
- •Contraception
- •Treatment of Endometriosis
- •Dysmenorrhea
-
Progestin Oral Contraceptives
- Category: Oral Contraceptives
- MOA:
- •Suppress ovulation
- •Diminish endometrial implantibility
- Unique Characteristics:
- •Often accompanied by spotting and bleeding
- •Available in depot forms for implantation
- •Side effects include headache, dizziness, weight gain
- Predictable Actions:
- •Useful in patients for whom estrogen is undesirable
- •Avoid side effects of estrogen including hepatic disease, hypertension and thromboembolism
- •Less effective that combination contraceptives
-
Prednisone
- Category: Glucocorticoid
- MOA: Modify gene transcription
- Unique Characteristics:
- •Short to medium acting
- •Strong anti-inflammatory effect
- •Orally effective
- •Modest salt retention activity
- Predictable characteristics
- •Protein, lipid and carbohydrate metabolism
- •Secondary followed by primary adrenal insufficiency with prolonged use
- •Side effects customary of all glucocorticoids
-
Calcium
- Category: Mineral
- MOA: Numerous effects in muscle, bone, cell membranes
- Unique Characteristics:
- •Incomplete absorption (30%) even in presence of Vitamin D
- •Calcium carbonate absorption requires stomach acid, Calcium citrate absorption does not
- Predictable Actions:
- •Calcium citrate perferred in elderly
- •Treat hypocalcemia
- •Treat and prevent osteoporosis
- •Constipation common side effect (Rx with fruits)
- •Interacts with some drugs
-
PLF of Alendronate (Fosamax)
- Category: Bone resorption inhibitors
- MOA: Prevent bone resorption by inhibiting osteoclasts.
- –Prevent attachment of osteoclast precursor cells to bone
- –Decrease metabolic activity of osteoclasts
- Unique characteristics:
- –Less than 5% absorbed from G.I. tract (less with food)
- –Must take 30 minutes before eating in morning
- –Half of absorbed drug deposited in bone
- –Adsorb to hydroxyapatite and remains in bone
- –Irritating to esophagus (erosions prevented by remaining UPRIGHT)
- Predictable characteristics:
- –Very long half-life (1 to 10 years)
- –Rx osteoporosis, Paget’s disease, hypercalcemia
-
Calcitonin
- Category: Bone resorption inhibitor
- MOA: Binds to receptors on osteoclasts inhibiting osteoclast activity
- Unique Characteristics:
- –Peptide secreted by parafollicular cells of thyroid
- –Administered parenterally or via nasal inhalation
- –Salmon calcitonin used and most potent
- Predictable actions:
- –Rx Osteoporosis, Paget’s disease, hypercalcemia
-
Glyburide
- Category: Oral Antidiabetic
- MOA: Increase secretion of insulin and decrease secretion of glucagon
- Unique characteristics:
- –Sulfonylurea
- –Effective orally
- –Frequent drug interactions: thiazide diuretics, ACE inhibitors, ethanol (disulfiram-like effect)
- –Metabolized in liver
- –24 hour half-life
- –Skin rashes (3% of patients)
- –Occasional cholestasis
- –Tachyphylaxis
- Predicted actions:
- –Treat type 2 diabetes
- –Daily doses typically adequate
- –May cause hypoglycemia
-
Rosigliazone
- Category: Oral Antidiabetic
- MOA: Decrease insulin resistance by regulating genes involved in glucose and lipid metabolism.
- Unique Characteristics:
- –Often used in conjunction with other oral antidiabetic agents
- –May cause fluid retention (edema)
- –Used in prediabetics to prevent diabetes
- Predicted Actions:
- –Treat type 2 diabetes
- –Slow onset (gene regulation)
- –Weight gain is common
-
Acarbose
- Category: Oral Antidiabetic
- MOA: Inhibit breakdown of polysaccharides in gut by inhibiting alpha-glucosidases.
- Unique Characteristics:
- –Target sucrase, maltase, glycoamylase, dextranase.
- –Defer digestion and absorption of sugars to distal small intestine
- Predicted actions:
- –Lower post-meal glycemic levels
- –Insulin sparing
- –Flatulence, diarrhea and abdominal pain
-
Testosterone
- Category: Androgen
- MOA: Bind to androgen receptor in nuclei to regulate protein synthesis.
- Unique Characteristics:
- –Converted to dihydrotestosterone by alpha reductase.
- –Metabolized in liver to measurable metabolites.
- –Some metabolized to estrogen.
- –Rapidly absorbed from G.I. tract
- –Used to treat endometriosis (especially Danazol)
- –Used in treatment of osteoporosis
- Predictable Actions:
- –Increased muscle mass
- –Contraindicated in pregnant women or women who may become pregnant
-
Finasteride
- Category: Antiandrogen
- MOA: Inhibit 5-alpha reductase to prevent conversion of testosterone to dihydroxytestosterone.
- Unique Characteristics: nothing remarkable
- Predictable Actions:
- –Diminish prostate size in BPH
- –Treat hirsutism in women
-
Actions of Vitamin D, Parathyroid hormone and Calcitonin
- Vitamin D (increases serum Ca)
- •Stimulates Ca absorption from G.I. tract
- •Stimulates bone resorption
- •Inhibit Ca excretion by kidney
- Parathyroid hormone or PTH (increases serum Ca)
- •Stimulates resorption of Ca by renal tubules
- •Decreases resorption of phosphate by renal tubules
- •Stimulate hydroxylation of vitamin D in kidney (active form)
- •Increases bone resorption by osteoclasts
- Calcitonin (decreases serum Ca)
- •Inhibits resorption of Ca from bone
-
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