Test II Flashcards by Rodrigo N

yes

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MOA: Non Selective 1st Generation H1 antagonist inverse agonist. Require multi daily dose. Anti-cholinergic/inflammatory

Indicx: Temporarily relives s/s of hay fever. Common cold, sneezing, runny nose, itchy eyes, itchy throat and nose.

AE: Anticholinergic effects, HYTN, Excitement in children. Caution: Glaucoma and BPH

Brompheniramine

Chlorpheniramine

Diphenhydramine

Promethazine

Hydroxyzine

Meclizine

Cyproheptadyne

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MOA: Non Selective 2nd Generation H1 antagonist inverse agonist. Daily dose.

Indicx: Temporarily relives s/s of hay fever. Common cold, sneezing, runny nose, itchy eyes, itchy throat and nose.

AE: Headache; Intranasal=Bitter taste.

Fexofenadine (Allegra): Non sedating

Loratadine: Non-sedating Pregnancy Cat B

Desloratadine (Clarinex)

Cetirizine (Zyrtec): Low sedating Prego Cat: B

Levocetirizine (Xyzal)

Azelstine (Astellin): Intranasal, Crosses BBB

Olopatadine (Patanese) : Intranasal Highly selective= Decreased AE

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ACOG Preferred H1 antagonist 1st Generation for pregnancy

Brompheniramine

Chlorpheniramine

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H1 antagonist 1st Generation used for N/V

Phenergan

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H1 antagonist 1st Generation used as sleep aid

High Anticholinergic and Sedative effect

Dyphenhydramine

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H1 antagonist 1st Generation

Indicx: Used primarily for urticarial and hives

Hydroxyzine

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H1 antagonist 1st Generation used primarily for vertigo

Meclizine

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H1 antagonist 1st Generation also has anti- serotonin properties

Indicx: Seratonin syndrome

Cyproheptadine

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MOA: Optic Direct and indirect A1 agonist producing vasoconstriction of respiratory mucosa.

Indicx: Congestion, Relaxes bronchioles, Inc. HR
Nasal/ Topical < than 3-5 days to prevent rebound congestion

DI: MOAi, AE: Incr. BP and HR, stroke, CNS stimulant, Caution: hyperthyroid, arrhythmia, HTN, BPH, Glaucoma

Oxymetazoline

Pseudoephedrine

Phenylephrine

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MOA: Direct acting A1 and A2 agonist produces vasoconstriction

Indicx: Relief of redness and congestion

AE: Stinging or burning

Oxymetazoline

Afrin/ Visine

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DOC in pregnancy second trimester decongestant

Pseudoephedrine

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Combo Allergic Rhinitis 1st Generation

Brompheniramine + PE (Dimetapp)

Carbinoxamine + PE (Rondec)

Chlorpheniramine + PE (Actifed)

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MOA: Decongestants that have minimal Blood pressure effects

Indcx: HTN patients w/ allergic rhinitis symptoms

AE: Abuse potential

Coricidin

Nasal Strip or Intranasal saline

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MOA: inhibits cysteinyl leukotriene Antagonist, inflammatory mediator by mast cell.

Indicx: comparable to A-histamine but less effective than INS

AE: Headaches, mood behavior changes, suicidal behavior

Montelukast (Singulair)

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MOA Irrigates and cleanses nasal passages of mucous

Indicx: All patients to include infants and pregnancy

AE: Infx from water organisms, irritating solution

Intranasal Saline (Sinus Rinse)

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MOA: Anti-inflammatory agents that inhibit the mediators released in both the early and late phase reaction

Indicx: Most effective Rx for allergic rhinitis. 1-2 days w/ max effects 1-2 weeks

(oral burst w prednisone 40mg/day for debilitating S/S)

AE: Drying/stinging nasal, Growth suppression, septal perforation. Epistaxis. DI: 3A4 Inhibitors

Intranasal Steroids

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INS with low systemic bioavailability

Fluticasone propionate (Flonase)

Fluticasone Furoate (Veramyst)

Mometasone (Nasonex)

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INS may exert significant systemic effects and decrease growth velocity

Beclomethasone

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INS preferred if pregnant

Budesonide

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INS Steroid exerts significant systemic effects

Flunisolide

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INS Combination

Indicx: Allergic Rhinitis 6 yrs and older who need both antihistamine and INS

AE: Somnolence/Drowsiness, epistaxis, nasal ulceration, impaired wound healing, candida albicans infx

Azelastine and Fluticasone propionate

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MOA: Anticholinergic muscarinic antagonist results in decrease mucous secretion.

Indicx: rhinorrhea

AE : Use <4 days, > 5 y/o patients

Ipratropium

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MAO: Inhibits Mast cells degranulation, prevents release of histamine and leukotrienes after contact w/ antigen

Indicx: Best use preventive S/S; DOC for pregnancy rhinorrhea and sneezing (Less effective therapy)

AE; Stinging/burning Nasal : Use 1-2 wks prior to S/S 3-4 TIMES DAILY DOSE

Cromolyn Sodium (Mast Cell Stabilizer MCS)

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MAO: Non selective 1st Gen H1 Receptor antagonist decreases itching and vasodilation (Tearing and swelling) Indcx: Itching red eyes Allergic conjunctivitis AE: stinging, burning, dry eyes, HA, bitter taste, Mydriasis and vision disturbances inc.IOP --> CI: Glaucoma

Azelastine Levocabastine

MOA: 2ng Generation competitive ocular H1 antihistamine Indicx: Popular and most effective, fast acting w/ prohylaxis

Ketotifen Olopatadine (Superior over Ketotifen)

MOA: A- agonist that constricts conjunctival vessels thereby reducing redness and swelling Indcx: Limit 3-5 days use Allergic conjunctivitis AE: Stinging burning, rebound hyperemia, mydraisis CI; Glaucoma

Ocular decongestants ``` Naphazoline, Oxymetazoline, Tetrahydrozoline Naphazoline + pheniramine (D Con + A-histamine) Naphazoline + Antazoline (Combo) ```

Ocular decongestant most potent

Naphazoline (Vasocon)

Long actin: Ocular decongestant causes more rebound Hyperemia.

Oxymetazoline (Visine LR

MOA: Ocular mast cell stabilizer stabilizes mast cell preventing degranulations and release of histamine and inflammatory mediators. Indicx; Slow onset of MC mediators: MC w/ a-histamine combo AE: Stinging and burning: Headache

Cromolyn Lodoxamide Nedocromil

MOA: NSAID decrease prostaglandin production Indicx: relief of pain, inflammation and itching AE: Stinging/burning, may induce asthma attack in patients w. ASA sensitivity

-Ketorolac

MOA: A-Inflammatory agent: Refer to opthamologist. Only approved steroid for allergic rhinitis Indicx: reserved for severe and chronic cases of allergic conjunctivitis AE: Cataracts, Increased IOP, Increase risk of ocular infx

Loteprednol (Ocular Steroid)

COPD non Rx treatments

Exercise Supple. O2 Reduce Exposure Vaccinations Pneumococcal and influenza

COPD Management

1 A. PRN SABA or SAMA (Short Acting Muscorinic A-gonist) 2B. 1st LAMA or LABA 2nd LAMA + LABA 3C. 1st LAMA 2nd LAMA + LABA 4D. 1st LAMA + LABA 2nd LAMA + LABA + ICS

MOA Short acting:B-2 Adrenoreceptor agonists increases cAMP in smooth muscle--> relaxation. Inhibits Mast cell mediators Indicx: PRN or 4 times/daily Long term tx of COPD (both)

Levabuterol (Metered dose Inhaler MDI) *Albuterol (MDI and Dry powder inhaler DPI) Neb, PO, Inj Terbutaline (DPI) PO and Inj.

MOA Long acting:B-2 Adrenoreceptor agonists increases cAMP in smooth muscle--> relaxation. Inhibits Mast cell mediators Indicx: LABA preferred to regular use of SABA: Long term tx of COPD

Salmeterol (MDI/DPI) Olodaterol (SMI) Soft mist inhaler *Formaterol (DPI) Nebulizer Indacaterol (DPI) *Aformeterol (Nebulizer)

MOA: Short acting Anticholinergic inhibits vagal mediated reflex. PreventsCa+2 by preventing interaction w M3 recep. on bronchial muscle. Indicx: COPD Bronchospasms; Not for acute episodes that require rapid response AE: Prego cat B: Sensitivity rx, A-cholinergic effects, Paradoxical bronchospasm

*Ipratromium Bromide (Atrovent) Nebulizer

MOA: Long acting Anticholinergic inhibits vagal mediated reflex. PreventsCa+2 by preventing interaction w M3 recep. on bronchial muscle. Indicx: Long Term once daily maintenance tx of COPD bronchospasm (Not for acute episodes) AE: Prego Cat C; Sensitivity rx, A-cholinergic effects, Paradoxical bronchospasm

Glycopyrronium Bromide : (DPI and MDI) PO and Inj Aclidinium Bromide; (DPI and MDI) Tiotropium: (DPI and SMI) Umeclidinium: (DPI)

MOA: SABA and SAMA Combination

Fenoterol and Ipratropium Albuterol and Ipratromium (Combivent)

MOA: LABA and LAMA

Formoterol and Glycopyrrium Indacaterol and Glycopyrrium Vilanterol and umeclidinium Olodaterol and Tiotropium

MAO: symptom relief that lead to hospitalizations; improves lung function QOL IndicxReduce exacerbations in Mod-Sev COPD. More effective component Combo w/ LABA AE: Thrush, dysphonia bruising, Red. Bone density, pneumonia. Rinse mouth/mouth piece w Each use

Inhaled Corticosteroids (ICS) Formeterol/Budesonide Formeterol/Mometasone Salmeterol/Fluticasone Vilanterol/Fluticasone

MOA: Causes bronchodilation, diuresis, CNS and cardia stimulation and gastric acid secretion. Blocks PDE Inc. CAMP--> release of epi from adrenal glands. Methylxanthine (Caffeine) Indicx: Adjunct to inhaled B2 Selective agonists Asthma and Chronic lung disease (Sytemic Admin:) No if LABA available W/ Salmeterol produces incr. in FEV 1 and improves breathlessness post -bronchodialator lung function

Theophylline Aminophylline

MOA: PDE4 inhibitor that reduces inflammation through inhibition of the breakdown of intracell cAMP no bronchodilator activity Indicx: Daily tx to reduce risk of COPD and exacerbations of COPD in pts w/ severe COPP FEV< 50% predicted COPD Gold 3-4 pts CI: Mod-Severe Liver disease: Nursing mother AE: Weigh loss, diarrhea,nausea, HA, Influenza DI: CYP450, CYP43A4 (Erythromycin, ketoconazole, cimetidine

Roflumilast (Daliresp) PO

COPD Exacerbations Short acting Low potency treatments

Hydrocortisone Cortisone Acetate

COPD Exacerbations Intermediate acting Med potency treatments

Prednisone Prednisolone Methylprednisolone Triamcinolone

COPD Exacerbations Lon acting High potency (Best anti inflammatory) treatment

Dexamethasone

Exercise Induced Bronchospasm Treatment

SABA (albuterol) 15 min. before exercise LABA (Salmeterol or Formeterol) 30-60 min prior exercise NO Leukotriene modifiers given daily should be used PRN before exercise

MAO: SABA B2 causes bronchodialation Inhibits mast cell mediators. Indicx: DOC for acute bronchospasm; EIB >2/wk =step up

Albuterol (Salbutamol) (Proventil) Levalbuterol (Xopenex)

MAO: LABA B2 causes bronchodialation Inhibits mast cell mediators. More effective w/ ICS in lieu of Inc. ICS dose Indicx: Long term effective Asthma control; NOT for acute excacerbations--> slow onset. Long duration AE: BB Warn: Incr risk of asthma related death

Folomoterol (Foradil) Salmeterol (Serevent Diskus)

MAO: Steroids :Antinflammatory, Block late reaction to allergen and reduce airway responsiveness. Inhibits leakage Indicx: 1st line most potent anti-inlammatory (reversal) reverse airway remodeling. Mild-Severe persistent asthma AE: Should not be used alone. Cough, dysphonia, thrush. Rinse mouth/mouthpiece

Beclomethasone Budesonide Ciclesonide Flunisolide Fluticasone MDI Fluticasone DPI Mometasone DPI

MAO: Antinflammatory, Block late reaction to allergen and reduce airway responsiveness. Inhibits leakage Indicx: Used for rapid response during exacerbation 1-3 onset peak 6-9 hrs Short courses used to grain prompt control most AE: Growth suppression,HPA suppression, cushing's, cataracts, impair immune; Weight gain, Incr. appetitie, HTN and peptic ulcer

Prednisone and Prednisolone MC: Methylprednisolone; I.V (ER) or no PO tolerance

Combine LABA Cortcosteroid Indicx: Long term prevention of S/S: Suppression, control and inflammation reversal. Reduce need for steroids NOT for acute symptoms

Fluticasone and Salmeterol Budenoside and Formeterols Mometasone and Formeterol Fluticasone Furoate and Vilanterol

MAO: Mast Cell Stabilizer prevents mast cell release of histamine and leukotrienes; Antiinflammatory blocks allergen rx Indicx: Alternative, not preferred tx of mild persistent asthma: Excellent safety profile; less effective than ICS AE: Cough and irritation and unpleasant taste

Cromolyn Sodium

MOA: Ani-Ige Monoclonal Anti-body, binds to circulating Ige prevents binding w basophils and mast cells Dec. Mast cell mediator release from allergen exposure Indicx: Moderate to severe Allergic sthma >12 y/o every 4-6 wks AE: Pain and bruising @ inj. site : Anaphylaxis .2% pts

Omalizumab (Xolair)

MOA: Inhibits Cysteinyl Leukotriene from mast cell on specific target cells LTC/LTD/LTE 4 Indicx: Long term control and prevention of symptoms in mild persistent asthma pts. Combo w/ ICS in mod persistent asthma AE: Headache, Mood behavior changes, discontinue if liver dysfunction

Montelukast Zafirlukast (Reversible Hepatitis) Monitor

MAO: 5-lipoxygenase inhibitor, inhibits leukotriene production from arachidonic acid; Leukotrine modifier Indcx: Long Term control of S/S in mild persistent asthma. Used w ICS combo; 2nd line agent. less effective than ICS DI: Anticoagulant effect of warfarin AE: Inc. Liver enzymes Monitor ALT CI hepatic fx impairment or incr. Etoh use

Zileuton

MOA: Bronchodialation via competitive inhibition of muscarinic cholinergic receptors Indicx: Alternative for SABA non tolerance patients Use w/ B agonist Combo in acute asthma exacerbation in ED or hospital Older pts and COPD pts. NOT EIB AE: Dry mouth, and resp. secretions, incr. wheezing and blurred vision if in eyes. ED; Less cardia stimulation than SABAs

Ipratropium Tiotropium

Improves pulmonary delivery and minimizes systemic or local AE: All patient w med-High dose ICS; and for pts w poor hand -lung coordination. Helps pt breathe at own pace

Metered Dose Inhaler Spacer

MOA: binds to nicotinic-cholinergic rec. adrenal medulla, NM junction, and brain Indicx: Tobacco sessation AE: HA, mouth irritation and dyspepsia, Throat irritation, cough, rhinitis (Inhaler)

Nicotine Gum: 2mg= <24Cgrt/day 4mg= >25 Cgrt/day Nicotine Lozenges: 2mg= 30min> after waking 4= < 30min. Nicotine patch: >10 Cgrt/day 21mg/day <10 cgrt/day14mg Nicotine Inhaler

MOA: Dopamine and norepi reuptake inhibitor w min. activity on serotonin AE: HA, insomnia, irritability, N/V, dec. appetite inc. risk of seizures: Suicide thinking behavior. psychosis hallucinations, anxiety aggression DI: MAOi

Bupropion

MAO: Partial A4 B2 nicotinic rec agonist; Prevents nicotine stimulation assoc. w nicotine addiction. Stimulates dopamine activity --> Dec. cravings Indicx: Smoke cessation AE:HA, insomnia, irritability, suicide ideation, depression N/V. Somnambulism. Harm to self, others and property

Varenicline (Chantix)

Hypothalamic-pituitary Adrenal Axis (HPA) is more likely to occur with

Prednisone > 20mgequivalent for > 3 wks Prednisone Taking > 5mg evening /bedtime for > 3 wks (Alternate day dosing to every other day)

Good lubricating properties ability to vanish into skin Generally less potent than ointments of same Rx Acute exudative inflammation responds well to this

Cream Topical Steroids

More lubrication and occlusion than other preparations More effective w/ dry heperkeratotic lesions Occlusive property inc. effectiveness NOT for hairy areas--> folliculitis

Ointment Topical Steroids

Least greasy and occlusive contain alcohol, useful for hairy areas dry easy exudative inflammation- poison ivy

Lotion and Gels Topical Steroids

Hair application effective Expensive

Foam mousses shampoos Topical Steroids

Method in which to determine topical steroid potency

Vasoconstriction assay

Topical: Do not discontinue abruptly , taper off w/ lower potency No > 2-4 wks continuous use Generally avoid occlusive dressing

Level I: Very high potency

occlusive dressings only to be used w/ Betamethasone

Level II High potency

Preferred w/ large body area well tolerated > 3mths use or less (Non facial Occlusive dressings: Only with Diflorasone Diacetate and Fluocinonide

Level III, IV and V : Medium potency

For children, pregnancy, elderly and large areas. Preferred for Face, groin, armpits, skinfolds

Level VI and VII Low

Very high potency Steroids

Clobetasol Propionate Augmented Betamethasone diproprionate .05% oint. Fluocinonide .1%

High potency steroids

Augmented Betamethasone Diproprionate .05% Lotion/cream Betamethasone Diproprionate .05% ointment Traimcinolone Acetonide .5% Fluocinonide .05%

Medium potency

Betamethasone Diproprionate .05% oint/cream Betamethasone Valerate .1%/.12% Traimcinolone Acetonide .025-.1% Hydrocortisone Valerate .2% Fluocinolone acetonide .025%

Low potency

Desonide .05% Hydrocortisone .5%, 1%, 2% and 2.5 % HydrocortisoneAcetate 1%

Most prescribed for short term therapy in inflammatory D/O Available in_____

Prednisone Tablets and syrup

Commonly prescribed for short term and is injectable as well as oral and syrup

Prednisolone

Available as 6 day 21 taper package, same efficacy as prednisone w higher cost

Methilprednisolone Tablets

Formulation for IM and joint injections

Methylprednisolone Acetate

Commonly used for asthma attacks and allergic reactions

Methiprenisolone Sodium Succinate

IM and joint injections tablets rarely used

Traimcinolone

Long acting oral Glucorticoids Allergic states, Respiratory disease Derm D/O, Endo D/O, GI D/O Ophthalmic or oncology for N/V

Dexamethasone

MOA: Potent nonselective inhibitor of adrenal gonadal steroid synthesis. Dec body production of corticoids; Antifungal Indcax: hyperadrenocorticalism (unapproved use) Cushinds disease when surgery not possible AE: Adrenal suppression, gynecomastia, hypercholesterolemia, hypothyroidism

Ketaconozole

MOA: Target distal tubule and collecting ducts in kidneys --> Na+, water and Bicarb reabsorption Indicx: Addison's disease Adrenals do not produce enough cortisone and aldosterone Supplement w/ hydrocortisone or Fludrocortisone

Aldosterone

MOA: Exogenous mineralocorticoids 15 times more activity than hydrocortisone Indicx: Replaces aldosterone in Addison's disease primary and secondary

Fludrocortisone

MOA: Aldosterone Agonist Indicx: Diuretic for CHF Tx primary Aldosteronism

Spironolactone and Eplerenone

Skin rate limiting step for percutaneous absorption extends halflife of medications (RESERVOIR)

Stratum corneum

Contact dermatitis Treatment irritant or allergic Goal: relieve itching, inflammation, protect skin integrity

1st remove offending agent Mild: Wet dressing: Dec pt itching Astringent: --> tissue contraction Dec. edema and inflammation. Oatmeal bathdries lesions and provides antipruritic effects Moderate: Camphor .1%-3% and menthol, Antihistamines Mild-mod topical steroid Severe= System corticosteroids prednisone 40 mg x4-6 days then 20 for 4-6 days taper off

Seborrheic Dermatitis treatment scaly patches, red skin, stubborn dandruff at scalp. Face upper chest and back (chronic D/O)

Ketoconazole shampoo Most effective Coal Tar, selemium sulfide, zinc pyrithione

Atopic Dermititis (Eczema) Pruritis of unknown origin (Allergy to food or environment) IgE mediated response to skin

Eliminate Allergen Cetaphil: Inc. skin hydration, Aluminum subacetate, Oatmeal Colloidal Corticoid steroid Med-High Topical Immunomodulators: Primecrolimus or Tracrolimus Oral antihistamines

MOA: Inhibit T Celll activation in inflamed skin by blocking transcription of pro inflammatory cytokines Indcx: Atopic Dermatitis Chronic inlafammatory disease. Psoriasis. Alternative to topical steroids. 1st line steroid sparing agent for face, flexural or genital area AE: Skin burning and warmth, skin infections, flu like s/s UV exposure cancer risk (BB Warn Skin cancer Lymphoma) < 6 weeks

Primecrolimus 1% Tacrolimus .03% TIMS

Impetigo Staph MC or streptococci. R/O Impetigo when evaluating contact dermatitis

Mupirocin DOC System Abx Dicloxacillin or cephalexin more effective than topical

Acne Rosacea: Unk cause Cheeks, nose and chin have a rosy hue, no comedones, burning stinging or flushing, 30-50 y/o Triggers= Hot liquids, spicy foods, alcohol sunlight and heat Tx;?

Metronidazole DOC Papulopustular rosacea Azelaic Acid (Mild-Mod rosacea) Sodium Sulfacetamide 10% and sulfur 5% Brimonidine .33 %: Persistenterythema of rosacea 18> y/o Ivermectin 1% cream: lice

MOA: Dual mode Releases O2, lethat to P. acnes and irritant increases epithelial cell turnover.resolution in skin Indcx: Acne Vulgaris non/inflammatory 50-75% red. in 8-12 wks esp. w erythromycin AE: Photosensitive, burning/stinging, drying/irritating of skin. Try low dose 1st

Benzoyl peroxide

MOA: Supresses P acnes which minimizes inflammatory response Indicx: Severe Acne Vulgaris most effective w Benzoyl Peroxide AE: Burning/irritation, pseudomembranous colitis > 8wks of admin

Clyndamycin 1% Erythromycin 2% Clindamycin and Benzoyl Peroxide Erythromycin and Benzoyl Peroxide (Peroxide red. risk of resistance)

ABX: Indicx: Acne Vulgaris prevents future lesions when topicals not tolerated or failed 4-6 mths and taper off

Tetracycline and Erythromycin rarely used due to Inc. resistance and GI upset Minocycline or Doxycycline: MC Bactrim: w resistance to Tetra and Erythro

MOA: Vitamin A analogs: reduces the production of sebum which is required by P Acnes. Inhibits neutrophil and monocyte chemotaxis Indcx: Acne vulgaris when Benzoyl and topical Abx fail AE: Dryness, redness and peeling of skin: darken skin and cause photosensitivity. Pustular flare x14 days begun acne worse 1st then but resolves PREGO C and X

Tretinoin: Prego C Adapelene: Prego C (Better tolerated and faster than Tretinoin) Tazarotene: Prego X (Psoriasis) Cream/Gel best efficacy Isotretinoin: Prego X (Degraded by UV use nightly)

Only effective agent in severe cystic acne vulgaris iPLEDGE registration: provider, patient, and pharmacy have to register to get the product AE: Prego Cat X: Two forms of contraceptive must be used. 1 mth post treatment: Cheilitis, Dryness of nasal mucosa, dry eyes, dark skin, alopecia, nail fragility depression and suicidal intentions

Isotretinoin (Accutane) PO

unknown, efficacy secondary to a combo of antimicrob activity against acne-related microorganisms and anti-keratinizing effects on the follicular epidermis Indicx: Rosacea or acne-comparable to Tretinoin, benzoyl, erythromycin AE: Pruritis, burning stinging, tingling

Azelex: 20% topical cream for acne vulgaris Finacea:15% topical gel for rosacea

MOA:Selective alpha-2 adrenergic agonist May reduce erythema through direct vasoconstriction Indicx:persistent (non-transient) erythema of rosacea in adults AE: Flushing 30min-hrs. BP lowering effect

Brimonidine .33%

Characterized by erythematous papules and plaques with a silver scale

Psoriasis

Psoriasis treatments combine or alternate w vitamin D analogues, tazarotene or emollient to improve efficacy Efficacy increases as potency increases AE: Skin atrophy Limit high potency to 2-4 wks

Topical Steroids 1st Line

Psoriasis treatment Mild-Mod plaque, less effective than steroids. Pts who need affordable tx Skin irritation, photosensitivity, non-pleasant odor, carcinogenic in animals

Coal Tar

MOA: in psoriasis is unknown Affect neuromuscular and immune function Slows skin cell growth, flatten lesions, remove scales Indicx: Mild Psoriasis monotherapy Severe in combo AE: skin discomfort, monitor calcium, not for use on face, flexures, genital use

Vitamin D3 Analogues Calcitriol 3mcg/g ointment (Vectical) Calcipotriol aka calcipotriene 0.005% solutions, ointments, foams (Calcitrene, Dovonex, Sorilux) Calcipotriene 0.005% and Betamethasone dipropionate 0.064% foam, ointment, suspension (Taclonex)

MOA: Topical Retinoid Vitamin A derivative Modulates differentiation and proliferation of epithelial tissue Reduces inflammation by inhibiting neutrophil and monocyte chemotaxis Indcx: Mild plaque psoriasis and acne Vulgaris AE:Local irritation CAN NOT be used on genitals or skinfolds Photosensitivity (Use sunscreen)Teratogenic risk

Tazarotene (Tazorac): Gel, cream , foam

MOA: Oral Retinoid Reduces inflammation by inhibiting neutrophil and monocyte chemotaxis Indicx: Psoriasis severe or extensive: Monotherapy or adjunct to phototherapy, Vit D analogues, steroids AE: Mucocutaneous dryness, alopecia, HIGHLY teratogenic. CI: 3 YEARS post discontinue

Acitretin PO

MOA: Inhibit T cell activation in inflamed skin by blocking transcription of pro-inflammatory cytokines Indicx: Atopic Dermatitis: Alt. To steroids. A first-line steroid sparing agent for atopic dermatitis and psoriasis of the face, flexural or genital area AE: skin burning, warmth, skin infx, flu like symptoms caution UV exposure BBW Lymphoma, skin cancer, use <6 weeks

Pimecrolimus 1% cream (Elidel) Immunomodulators (TIMS) Tacrolimus 0.03% ointment (Protopic

MOA: Folic acid antagonist, inhibits purine synthesis by acting on dihydrofolate dehydrogenase Indicx: Disease that is too severe, refractory, or extensive for topicals: soles, scalp or inc. body surface AE:

Methotrexate

MOA: a microemulsion forming formulation that minimizes intra-individual absorption variability Indicx: Disease that is too severe, refractory, or extensive for topicals: Palms, soles, scalp use in combo w Vtamin D3 analogues and steods AE: Use is limited due to effects and interactions; Nephrotoxicity, skin cancer, HTN, Hyper TGC

Cyclosporine PO

MOA: Phosphodiesterase 4 (PDE4) Inhibitor Reduction of inflammatory mediators. Nitrous oxide synthase expr Indicx: Psoriasis Mod-severe in phototherapy and systemic therapy candidates; No lab monitor required Less efficacy but less AE: AE: NVD, weight loss, Dperession suicidal, HA, URI, DI CYP3A4

Apremilast (Otezla)

block pro-inflammatory cytokines TNFα, interleukin (IL), bind on target receptors on T-cells prevent stimulation activate T-cells Indicx: Most Effective Agents for Psoriasis Mod -severe psoriasis AE: risk of lupus, TB, Demyalinating D/O cancers Less toxic to kidney, liver and bone marrow than methotrexate

Infliximab (Remicade): Chimeric antibody to TNF-α (MOST EFFECTIVE) Adalimumab (Humira): Human IgG antibody to TNF-α Etanercept (Enbrel): TNF-α antagonist Ustekinumab (Stelara): Human antibody to IL-12 & IL-23

Wart Treatments Physical destruction of affected tissue 1-2 wks improvement resolve 4-6 weeks

Slaycilic Acid 17% liquid 40% plaster

Wart tx. plant resin causes mortality of effective cells Indicx: external warts only; Applied daily x3 days stop 4 days and repeat 4 tmes AE: necrosis of healthy skin, pain infx, irritation CI: Prego X toxic to fetus

Podofilox Podophyllum

MOA: Green tea leaves. Upregulate apoptosis associated genes. doulate down regulate genes involved inproinflammatory response to HPV Indicx Warts; Placebo 55% cost 200 Dlrs/tube

Sinecatechins

Releases progestin in uterus | Remain in place for 3-5 years

Intrauterine device

Thin, flexible, 2 inches in diameter Delivers synthetic estrogen and a progestin analogs for 3 weeks Remove for 4th week, insert new ring 7 days later AE: High estrogen content increases risk of blood clots, stroke, heart attack, or cancer. Avoid if pt. has history

Vaginal Ring

Matchstick-sized rod placed under the skin of the upper arm -Releases a low dose of progestin (60-70mcg)--> 35-45 mcg --> 30-40mcg --> 25-30 mcg thrd year - Protects for up to 3 years - Requires local anesthetic for insertion

Birth Control Implant Implanon Nexplanon

Injection Given in arm or buttocks once every 3 months (IM vs SubQ) Should eat diet rich in calcium and vitamin D In adolescents can cause temporary loss of bone densit Bone loss occurs during two years of therapy

Medroxyprogesterone

Signals growth of uterine lining in first part of menstrual cycle. Binds breast, uterus, bone, liver, heart, brain Causes changes in breasts during adolescence and pregnancy Regulates metabolic processes (i.e., bone growth and cholesterol levels) Suppress LH and FSH release

Estrogens Ethinyl Estrogen Estradiol Valerate Mestranol

Estrogen hormones type and what effects

Estradiol - Ovaries Estrone - ovaries Estriol- Placenta druing pregnancy

Suppress release of LH and FSH from pituitary gland via negative feedback by providing exogenous estrogen/ progesterone Prevent fertilization or abort implantation. Regulates hormones, relieves menses caramps, reduces heavy bleeding, reduces cancer, acne, ER contraception WITHIN 72 HRS

COmbined oral contraceptives

Combined Oral contraceptive types Constant dose of estrogen and progestin daily Avoids mood changes, dysmenorrhea, menses discomfort, ovarian cysts Indicated for Progestin dominance requirements

Monophasic

Combined Oral contraceptive types Two combinations of estrogen and progestin Example: estrogen amount is the same and progestin dose increases during 2nd phase of the cycle Positive in Acne Tx

Biphasic

Combined Oral contraceptive types Hormone dose changes every 7 days during 1st three weeks. Usually use a gradual increase in estrogen Ideal for complaints of progestin AE: like Increased appetite, acne, weight gain, CVD, or metabolic D/O --> Confusion color codes makes the missed dose instruction complicated

Triphasic

Combined Oral contraceptive types Hormone levels change four times per cycle Developed to reduce the side effects of OC Reduced OC AE: --> Confusion color codes makes the missed dose instruction complicated

Quadriphasic

Combined Oral contraceptive types Used for 84 days then 7 days placebo (91 days) Most are monophasic, but some newer ones are bi, tri or quadripasic

Extended Cycle

Combined Oral contraceptive types Monophasic OCP that does not have placebo days at all

Continuous Cycle

Estrogen and venous thromboembolism (VTE) Related to the estrogen dose Very low dose? Low Dose? High Dose? Starting dose EE w progestin?

VLD= < 30 mcg LD= ,30-50 mcg HD>= 50mcg Start= 20mcg

dosing initiation? More successful in getting women to start and minimizes confusion about when to start Take 1st tablet ASAP regardless of cycle day. Use alternate contraception method for 7 days

Quick Start (start at time other than post-menses)

First tablet on the first Sunday after the beginning of menstruation If menses starts on a Sunday, the first tablet should be taken that day Use alternative method of contraception for at least 7 days, most conservative for month

Sunday Start (Most Popular method)

First tablet on the first day of menses Most package inserts state that backup contraception is not needed with this method

First /Same day start

Missed doses with COC 1 hormonal dose <48hrs

Take late or missed pill asap No additional contraceptive or ER CC needed

≥2 consecutive hormonal doses have been missed | >48hrs

Take missed asap Use backup CC condoms or abstinate until 7 days of CC taken; ER CC; consider if during 1st week

If doses were missed during the 2nd or 3rd week of the current pack (i.e., days 15-21 for 28-day pills packs)

Discard the placebo week and start a new pack immediately after the last active dose unable to start- use backup CC or abstinence until 7days of new package CC taken: ER CC consider

Also known as the Mini-Pill only in 28 day pack. Must take 1 daily for 4 weeks. No placebo pills MUST BE taken within 3 hour window for effectiveness Indicx: Breastfeeding, just gave birth, Migraines, CVD, >35 and smokes, and HTN AE: causes hostile environment, thickens cervical mucus

Only Progestin Contraception

Progestin only CC Start method and Missed doses?

Quick Start on any day of her cycle, use back up CC x48hrs 1st same day start: Same day period starts= no backup CC needed Can take immediately post partum if not breast feeding; if Breastfeeding wait 3 weeks (6 weeks if solely Breastfeeding) Misses doses: use backup for 48 hrs

AE: spotting and irregular vaginal bleed, amenorrhea, HA, long periods. Loss Libido, increase or decrease acne mood changes, bone and hair loss, increase or dec. in body hair, 2 lbs weight gain

Progestin

Advantages and disadvantages of progestin

Advantages: Fertility returns quickly, preferable in lactating women, no placebo week and all pills the same. PID protection and Endometrial cancer Disadvantages: short window for missed pills, must take regularly, not used in none breast feeding

Low progestin activity and slight estrogenic affects - High risk of unscheduled bleeding and spotting - 2nd most androgenic

1st Generation Progestin CC

- More potent and longer half-life than 1st generation - MOST androgenic (antiestrogenic) activity Improved libido, but also associated with hirsutism, acne, and dyslipidemia

2nd Generation Progestin CC

Similar progestin activity as 2nd generation -Less androgenic (anti-estrogenic) activity Beneficial in patients with acne Associated with slightly higher risk of thrombosis

3rd generation Progestin CC

Least potent anti-mineralocorticoid and anti-androgen effects of spironolactone - Parent compound is spironolactone - Concerns of increased risk of venous thromboembolism

4th Generation Progestin CC

Delivers 35 mcg of ethinyl estradiol and 150mcg norelgestromin 60% more estrogen exposure than a 35mcg oral tablet of ethinyl estradiol Efficacy: Similar to pills Less effective in women weighing more than 198lbs (90kg), should NOT be used AE: COntact dermatitis, rotate sites. embolism risk higher. patch >24hrs use backup CC

Transdermal Patch (Ortho-Evra)

COC: 15mcg ethinyl estradiol and 120mcg of etonogestrel daily Efficacy: Similar to OCP (8% failure rate for typical use, 0.3% for perfect use) Administration: Insert vaginal ring into vagina and leave for 3 weeks Week 4 remove ring and menses will begin Should NOT be removed during intercourse May be worn with tampon if there is breakthrough bleeding Ring SHOULD NOT be promoted for use beyond 21 days

Vaginal ring

Missed doses for vaginal ring includes

Missed Doses: 3 hours or less: rinse with cool to lukewarm water and reinsert as soon as possible >3 hours: reinsert and use a back-up method until ring has been used continuously for 7 days

150 mg IM 104mg SubQ (Depo-subQ Provera) Clinical Use: contraception and endometriosis Don't massage area, expect irregular bleeding take calcium- return for next inj. 11-13 weeks. AE: Weight gain, delayed fertility 18 mths, dec. bone density do not use> 2 yrs

Depo-Medroxyprogesterone Acetate (DMPA

Recommended for no hx of PID or ectopic Prego, heavy menses, cramps anemia, 2 > Prego protection Cannot tolerate Estrogen Oral CCs Had atleast 1 child

Intrauterine Devices

MOA: Copper ions inhibit sperm motility and acrosomal enzyme activation so that sperm seldom reach fallopian tube and are unable to fertilize the ovum CI: allergy to metal, uterus <6cm or >9cm, abnormal vag bleeding, suspected cancer, risk STDs, Doc must insert

Copper (Paragard)

MOA: Foreign object in uterus, prevents implantation Thickens cervical mucus, thins endometrium, and inhibits sperm motility. Has lovanogestrel (progestin) CI: Acute hx of PID, multiple partners, endometriosis or abortion in past three mths

Mirena (5 years in uterus) Skyla (3 years in uterus)

Management of adverse effects Breakthrough Bleeding (BTB)

- BTB early in the cycle: not enough estrogen; select a regimen with higher estrogen activity - BTB late in the cycle: not enough progestin; select a regimen with higher progestin - Assess adherence; consider switching after trying for 3 months

Management of adverse effects Nausea and vomiting

- Related to estrogen component - Take at night before bed or with largest meal of the day - Nausea and vomiting may subside after a few months

Management of adverse effects Acne and Hirsutism

- Related to the androgenic properties of progestin - Select a progestin product with lower androgenic activity - Alternatively, select a product with a lower progestin component

Comorbid CC conditions cautions

Smoker > 35= CVD risk MI HTN= Estrogen Increases BP Hyperlipidemia= COC thromboembolic, incr TGC levels progestin Increases Progestin levels Migraine- risk of stroke w aura 2-4 Inc. srtoke

Inhibits ovulation, prevents fertilization, prevents implantation: not an abortifacient, not disrupt implanted egg Indicx: After intercourse to prevent pregnancy Should not be used as a routine method of contraception Less effective than other methods

Plan B : take within 72 hrs single or BID 1.5 mg/day OTC Ella: RX only : W/in 120 hrs 42% more effective than Plan B

Specific number of pills taken ASAP after unprotected intercourse Second dose 12 hours later AKA Yuzupe Method High dose-estrogen plus progestin

Monophasic COC Rx only

Time to fertility COC= Injectable DMPA= BC Implant=

COC= 1-3 mths Injectable DMPA= 10 mths post injection BC implant = 1 month after removed

BC post pregnancy Breast feeding

Progestin-only oral contraceptives or depot medroxyprogestin (DMPA) can be initiated at 6 weeks postpartum in lactating women

BC post pregnancy Not breast feeding W/O CV risk

Progestin-only oral contraceptives or DMPA can be initiated immediately postpartum in non-breastfeeding women Avoid estrogen containing products for initial 21 days Risk factors of thromboembolism

BC post pregnancy Not breast feeding W CV risk

Avoid estrogen-containing contraceptives for 42 days after delivery

Drugs that Interact w CC

Benzos and anticonvulsants or increase (AC/DC) decrease (LOT) Corticoids Increase Opiods decrease: Tricyclic A-depressants- increase Abx and supplements decrease (use alt method of cc) Rifampin

Relieves genitourinary atrophy; reduces pain with sexual intercourse Indicx: Women w/o uterus (w uterus include progestin) helps lower risk of thrombosis or stroke, less lipid effect - Relieves vasomotor instability - May help improve sleep by decreasing hot flashes - Osteoporosis: reduces resorption rate AE: CV, cancer (breast/Endometrial and thrombosis

Estrogen Menopause Therapy Medroxyprogesterone: Protects against carcinoma (Bloating, weight gain, depression) Micronized progesterone: equal to above at preventing hyperplasia

Menopausal therapy duration

Lowest dose for least time short term= 2-3 years no more than 5

Menopausal hormone Therapy Continuous estrogen daily Estrogen on calendar days 1-25 Medroxyprogesterone 2.5mg on day 14-25 Hold hormone therapy from day 26 to the end of the month

Estrogen + cyclic Progesterone

Menopausal hormone Therapy Continuous estrogen daily Continuous progesterone without interruption None or irregular menstrual cycle for the first 8-12 months of therapy

Estrogen + continuous Progesterone

Menopausal hormone Therapy Continuous estrogen daily Progesterone: 3 days on, 3 days off Not used often

Intermittent

Vaginal Estrogen products for atrophic vaginitis due to decrease estrogen secretion post menopause

Vaginal creams; local Vaginal Rings- Femring only one has systemic effects Vaginal Tablet: local Transdermal patches; local

Selective Estrogen Receptor Modulator (SERM): estrogen agonist/antagonist Bazedoxifene acts as an agonist of estrogen receptors in some estrogen sensitive tissues and an antagonist in others Indicx: Post-Menopause Osteoporosis Vasomotor symptoms AE: CVD, Malignant neoplasms, gall bladder disease, significant osteoporosis risk

Conjugated Estrogens/ Bazedoxifene (Duavee)

Non-hormonal Options for Menapause

vaginal lubricants: Selective Estrogen Receptor Modulators (SERMs) (raloxifene) SSRIs; Best for vasomotor symptoms in high-risk women for who HRT is not recommended Paroxetine mesylate SNRIs: Venlafaxine Clonidine, Gabanpentin, Methyldopa

estrogen agonist to improve lipid profile, decrease bone resorption, increases risk of thromboembolism and endometrial hyperplasia Works as an estrogen antagonist to reduce the chance of breast cancer AE: CV risk: Stroke, DVT and PE Endometrial cancer

Ospemifene (Osphena) PO Tamoxifen (Nolvadex) PO Raloxifene (Evista) PO

MOA: estrogen agonist to improve lipid profile, decrease bone resorption, increases risk of thromboembolism and endometrial hyperplasia Indicx: Mod-severe dyspareunia due to vaginal atrophy AE: CV risk, Hot flashes, Endometrial cancer

Ospemifene (Osphena)

Clinical Use: Approved for the treatment of breast cancer and prevention of breast cancer in high risk women Not approved for osteoporosis. AE: Hot flashes, Risk of VTE, endometrial hyperplasia

Tamoxifen

estrogen agonist to improve lipid profile, decrease bone resorption, increases risk of thromboembolism and endometrial hyperplasia Indicx: Prevention and treatment of osteoporosis in: High risk of breast cancer: cannot take biphosphanate dec. CAD risk CI: patients w VTE DI: warfarin, bile acid resins, thyroid hromones

Raloxifene

MOA: Mediates ovulation through increased output of pituitary gonadotropins indicx: Treatment of ovulatory failure in women desiring pregnancy Unlabeled use: used to treat male infertility AE: blurring spots or flashes, GI, ovary enlargement, multiple fetuses

Clomiphene

MOA: Inhibits the production of estrogen by blocking aromatase. Ring distinguishesestrogen from prog./Andr Indicx: indicated for advanced treatment of estrogen dependent breast cancer

Letrozole Anastrozole Exemestane

MOA: inhibits progesterone activity; also binds to glucocorticoid receptors Termination of intrauterine pregnancy; up to 70 days of gestation or Hyperglycemia in patients with Cushing syndrome

Mifepristone

stimulate protein synthesis Stimulates the production of red blood cells in patients with refractory anemia, particularly those with renal disease Indicx: Senile Osteoporosis and anemia: Testicular insufficiency impotence: Hypogonadism, delay of growth Female: hypopituitarism w estrogen metastatic breast cancer and endometriosis

Androgens

AE: Increase LDL decrease HDL CV risk and edema: Azoospermia (absence of viable sperm), impotence, prepubertal_ closure of growth plates Females masculinization, acne , face hair deep voice, male baldness, Inc. muscle

Androgens Anabolic steroid (Schedule III drug)

Indicx: promote weight gain where protein breakdown is part of the underlying condition

Oxandrolone Androgens

Androgen PO for Anemias from deficient RBC production

Oxymethalone

MOA: Androgen Derivative: synthetic androgen Indicx: Used to treat endometriosis and fibrocystic breast disease

Danazol

MOA: α blockers: block the α1 mediated contraction of the bladder neck - proven to decrease S/S in BPH Indicx: Obstructive: hesitancy, decrease force, incomplete voiding, and straining to urinate Irritative: urgency, frequency, and nocturia

Terazosin (Hytrin) and Doxazosin (Cardura): for BPH and hypertension Alfuzosin (Uroxatral): approved only for BPH Tamsulosin (Flomax): α1a selective approved only for BPH

Competitive inhibitor of 5α reductase. Halts BPH Indicx: progression and reduces prostate size and symptoms over time. Male pattern baldness. Hirsutism in women AE: decreased Libido, E-Dysfunction, ejaculation Dfx Prego cat X

Finestaride (Propecia)

MOA: Phosphodiesterase type 5 (PDE-5), is responsible for degradation of cGMP in the corpus cavernosum Indicx: E-dfx, Pulmonary Arterial HTN, BPH

Sildenafil: Viagra (4hrs duration) (nephrotic and liver impairment) Vardenafil: Levitra/Staxin (Liver impairment) Tadalafil: Adcirca/Cialis (36hrs) Avanafil; Should not be used CrCl<30 or hemodyalisis or severe hepatic impairment

FDA-approved: | Androgens:

Fluoxymesterone Methyl testosterone Testosterone enanthate Testosterone propionate Alprostadil (Caverject, Edex, Muse)

``` Prostaglandin E1 (PGE1) Causes vasodilation by means of direct effect on vascular and ductus arteriosus smooth muscle; relaxes trabecular smooth muscle by dilation of cavernosal arteries ``` indicx: erectile dfx establish dose in clinic then home admin

Alprostadil ( Penile injection) Urethal pellet available

Female sex dysfunction

Androgens Flibanserin (Only approved med) Zestra oil on Clitoris Dopamine agonist (Women w Parkinson)

exhibits serotonergic and dopaminergic activity Agonist activity at 5-HT1A Antagonist activity at 5-HT2A Moderate antagonist activity is seen at the 5-HT2B, 5-HT2C, and dopamine D4 receptors Indicx: Treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder AE: Dizziness, drowsiness, HyTN syncope: take at bed time

Flibanserin (Addyi)

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