Pharm II: Block 1 Flashcards
Which neuromuscular blocking agent is the DOC in renal/hepatic Dz?
What neuromuscular blocking agent is metabolized into Laudanosine?
Cisatracurium
Atracurium
Define Acute Pain
Self limiting/nociceptive result from injury
Define Non-Cancer Chronic Pain
Nociceptive, neuropathic or both that impacts daily living and persists greater than 3mon
Define Chronic/Malignant Cancer Pain
Life threatening condition pain w/ multi-modal cause
What are the 5 steps of the pain process?
Transduction- damage creates AP in peripheral nerve
Conduction- AP activates Na channels
Transmission- peripheral to CNS by primary afferent nociceptor
Modulation- reduces transmission via downward projection
Perception- awareness produced by sensory signals
What types of medications stop ascending pain pathways?
What types of medications stop descending inhibitory pathways?
Aspirin, Non-opioid analgesics
Opioid analgesics
Describe the Inflammatory pain process?
Protective and assists w/ healing by discouraging use
Activates immune system
Tenderness promotes repair
Stimulated by Macrophage, Mast, Neutrophil, Granulocytes
What classes of drugs are used to alter the perception of pain in the brain?
Opioids
A2 agonists
TCAs
SSRI/SNRI
What classes of drugs are used to alter the modulation of pain in the descending modulation?
TCAs
SSRI/SNRI
What classes of drugs are used to alter the transmission of pain in the dorsal root ganglion?
What classes of drugs are used to alter the transmission of pain in the peripheral nerve?
LAs, A2 agonists
LAs, Opioids
What classes of drugs are used to alter the transduction of pain in the peripheral nerve?
LAs Capsaicin Anticonvulsant NSAIDs ASA Acetaminophen Nitrate
What 5 classes of drugs can be used as adjuvant agents to reduce opioid burden?
TCAs- Amit, Nortri, Desipramine SSRI/SNRI- Dulox, Venlafax, Milnaciparn Anticonvulsant- Gaba, Pregaba Local anesthetic- Lidocaine Counter irritant- Capsaicin
Where are COX 1, 2 and 3 most commonly found?
COX-1= platelets, stomach and endothelium COX-2= inflammatory cells and kidneys COX-3= CNS (thermoregulatory control)
What are the undesireable and desired effects of COX-1 and COX-2 inhibition?
COX 1= Undesired= gastrotoxicity, Desired= antithrombic
COX-2= Undesired= HTN, Na retention, prothrombotic, Desired= anti-inflammatory, analgesic
What is the primary route of Acetaminophen metabolism?
What is the secondary route and what is adversely formed?
Glucuronidation and Sulfation to renal
3A4, 2E1, N-hydroxylation
Produces NAPQI- normally combined w/ glutathione and excreted renally
What three types of PTs/scenarios are at an increased risk of forming NAPQI?
Supratherapeutic doses (+4gm/24hrs)
Heavy alcohol/liver Dz (>3 drinks/day)
Malnutrition/Fasting
What are the three phases of an acetaminophen OD?
First 24hrs- GI Sxs, N/V
24-72- abd pain, liver tenderness, inc transaminase, decreased urine, jaundice
4 - 14 days- resolution or liver failure to death
What is the antidote to an Acetaminophen OD?
Charcoal regardless of lab wait times
N-acetylcysteine- metabolizes acetaminophen to cysteine which is glutathione precursor
Acetadote- injectable
Mucomyst- inhalation
N-Acetylecysteine is used in PTs w/ probable hepatotoxicity in what scenarios?
Single ingestion 150mg/kg or 7.5g total regardless of weight
Unknown ingestion time and >10mcg/mL
Hx of APAP ingestion and any evidence of liver injury
PTs w/ delayed +24hrs presentation w/ lab evidence of liver injury
What’s the max dose of acetaminophen per day?
Adults- max 3gm/day Elderly- <2gm/day Acetaminophen/opioid combo- 325mg/pill Infants/Children- 160mg/5ml Children Melt Away- 80mg Children- 10-15mg/kg/dose Q4-6
What is Aspirin’s effect on platelets?
What are the external uses of aspirin?
Anti-platelet due to irreversible COX inhibition
Salicyclic acid- acne, corns, callus, warts
Methyl salicylate- arthritis, sports rubs
As selectivity for COX 1 increases ? changes?
As selectivity for COX 2 increases ? changes?
Platelet aggregation is more prominent
Beneficial effects of platelet aggregation decrease, more CV risk
What is the list/precedence of treatment for PTs w/ CV Dz needing pain control?
Acetaminophen Aspirin Tramadol Opioids- short term Non-acetylated salicylates NSAIDS w/ low COX 2 selectivity NSAIDS w/ some COX 2 selectivity COX 2 selective agents
What type of PTs are at high risk of developing ulcers from NSAIDS?
Which ones are at moderate risk?
High- Hx of complicated ulcer
Mod- +65y/o, high dose NSAID, uncomplicated ulcer Hx, concurrent use of aspirin, corticosteroids, or anticoagulatns
PTs w/ low, moderate or high CV and/or GI ulcer risks receive what treatment regiments?
High CV, High ulcer= only alternative therapy
High CV, mod/low ulcer= Naproxen and PPI/Misoprostol
Low CV, High ulcer= alternative therapy or COX-2 inhibitor and PPI/Misoprostol
Low CV, Moderate ulcer= NSAID and PPI/Misoprostol
Low CV risk, Low ulcer= NSAID only at lowest effective dose
What are the 3 phases of Salicylate Toxicity?
1- N/V, tachypnea, HA, tinnitus; <150mg/kg
2- metabolic acidosis, respiratory compensation; 150-300mg/kg
3- sever K and BiCarb depletion, dehydrated, metabolic acidosis/respiratory compensation; >300mg/kg
How is Salicylate Toxicity treated?
No antidote Primary treatment= replenish BiCarb Activated charcoal and lavage O2 and E+ Glucose if AMS despite glucose levels Start dialysis
What are the pros and cons of using non-acetylated salicylates?
Effective anti-inflammatory Effective analgesics Less effect on platelets Lower GI bleeds Less renal toxicity
Con- less analgesic effect than aspirin
When is the use of non-acetylated salicylates preferred?
COX-1 inhibition needs to be avoided
PTs w/ asthma
Thrombocytopenia
Renal dysfunction
What are the uses and contraindications of using Ketorolac?
Decreases opioid requirement by 25-50% when treating mild-mod pain for less than 5 days
Cataract extraction, refractive surgery, ocular itching from allergic conjunctivitis
Don’t use in peds PTs, bleeding risk, w/ NSAIDS, renal impairment, Delivery
PBNDR
What is the max amount of Ibuprofen for adults and kids per day?
3200mg
2400mg
What effects do prostaglandins have in the eyes?
Meiosis
Increased vascular permeability in blood-ocular barrier
Pressure changes
What are the three ocular NSAIDS and their uses?
Flurbiprofen- inhibits operative meiosis
Diclofenac- post-op inflammation and photophobia
Keterolac- ocular itching and post-op inflammation
What type of NSAID is best for PTs w/ renal insufficiency?
Which one has the least CV events?
Which one has the lowest GI bleeds?
Non-Acetylated salicylates
Naproxen
Celecoxib
What effect do endogenous opioid peptides have on opioid receptors?
Opioid receptors= GPCRs
Peptides bind and inhibit adenylyl cyclase by controlling ion gating
What does a decreased amount of Ca2 influx in the presynaptic cleft do to pain?
Inhibits nociceptive input from periphery to spine
Activates descending inhibitory paths
Alters limbic activation
What medications inhibit the ascending pain pathway from nociceptors?
What medications inhibits the descending pain pathway?
Aspirin and non-opioids
Opioid analgesics
What are Mu, K, D and K receptors and their location?
Mu- most analgesic properties; U1- analgesia, U2- respiratory depression, sedation, euphoria
K- contribute to analgesic properties
D- located peripherally and selective for enkephalins
Opioid receptors are located in what three areas of the body?
CNS
Peripheral nerves
GI tract
Functions of Mu receptors
Supra/spinal analgesia, sedation, inhibits respiration, slowed GI motility, modulates hormone/neurotransmitter release
Functions of D receptors
Supra/spinal analgesia
Modulates hormone/neurotransmitter release
Function of K receptors
Supra/spinal analgesia
Psychotomimetic effects
Slows GI transit
Define Physical Dependence
Define Addiction
PTs use of drug is required for well being
Loss of control over drug use
Define Pseudo-Addiction
Under treatment of chronic pain leading to addiction-like behavior
What are the S/Sxs of opioid withdrawal?
CACAIN Anxiety Irritability N/V/D Chills, aches, cramps
CNS excitation from opioids is from the stimulation of ? receptor?
The use of ? drug can cause myoclonus/seizure like activity in renal failure PTs
Kappa- causes dysphoria
Meperidine- Demerol
What side effect to opioid use does not go away with tolerance/continued use?
What can be used for the adverse nausea effect of opioids?
Miosis, constipation
Corticosteroid
Antihistamine,
Metoclopramide
Serotonin antagonist
What three opioids are most likely to cause allergic reactions?
What two have fewer histamine related reactions?
Codeine, Morhpine, Meperidine
Oxy, Fentanyl
What are the Sxs of Opioid Allergy
What are the Sxs of Pseudoallergy and what drug is most likely to cause it
IgE/T-Cell induced hives, rash, erythema, HOTN, bronchospasm, angioedema
Flush, Itch, Sweats, Hives, HTON
Morphine
What are Sxs of opioid toxicity?
Confusion, Hallucinations, Agitation, Respiratory depression, Dreams
Caution is needed when using opioids for ?
Pure with weak agonists Head injuries Pregnancy Pulmonary, liver, renal impairments Endocrine dz
What is the most common used opioid used as prescription to suppressive the cough center of the brain?
What is the OTC derivative of this drug?
Codeine
Dextromethorphan
What is the least lipophilic of the common opioids prescribed?
Morphine- small amount crosses BBB and will cross placenta
What two drugs can be given if PT has adverse reactions to morphine?
Diphenhydramine
Hydroxyzine
How are the pharmacokinetics of Hydromorphone better than morphine?
Can all providers prescribe hydromorphone?
Better PO absorption, more fat soluble
Extended release is REMS drug, requires training Q2yrs
What is the sequence of best to worse binding affinity of morphine and it’s derivatives?
Hydromorphone
Morphine
Hydrocodone
What is Oxycodone metabolized into?
What is so special about polyethylene oxide form of oxy?
Noroxycodone and oxymorphone
Turns gummy when contacts w/ water
What are the adverse effects of mixed opioid ant/agonists?
Psychomimetic response
Precipitates withdrawal
Ceiling effect on respiratory/analgesic
Lower abuse potential
When are Fentanyl patches indicated for use?
Severe chronic pain PTs w/ opioid tolerance of +1wk on: >60mg Morphine/day >30mg PO Oxycodone/day >8mg PO Hydromorphone/day
Characteristics of the Fentanyl derivatives Alf/Suf/Remifentanil?
All three share what characteristics?
Alf- rapid onset/short duration
Suf- slower onset than Fentanyl but lasts same time
Remi- rapid onset but shortest duration, ONLY available by infusion
No infusion accumulation
What drug is classified as a Diphenylheptane?
What two drugs are classified as Benzomorphans?
Methadone
Pentazocine and Dipenoxylate
What types of PTs can not receive Tapentadol?
In order for Naloxone to have a systemic effect in can’t be taken through what route and but when it is, what for?
Renal dysfunction
Not systemic if PO- opioid induced constipation
Consider giving Naloxone to what PTs?
Hx of Intox/OD Suspected Hx of abuse/non-medical use Methadone/Buprenorphine use d/o >50mg of PO morphine or equivalent Rotated from one opioid to another Smoke, Respiratory, Hepatic, Renal, Heart, Alcohol, Benzo, Sedative, Anti-Depressants
When should Naloxone be given to a suspected OD PT?
Respiratory/CNS depression Pinpoint pupils in difficult to arouse PT Cyanosis Death rattle Bradycardia/HOTN
What is the MOA of Naltexone
What is it used for?
Mu competitive antagonist that competes but doesn’t displace opioids
Longer duration for opioid/alcohol dependence
What is the sequence of most hydrophilic to most lipophilic opioids?
Morphine Oxycodone Oxymorphone Hydromorphone Methadone Fentanyl
What are the two combo forms of Naltrexone and their use?
What are the contraindications for using Naltrexone
Morphine- post-op pain w/out abuse potential
Buproprion- weight management
Opioid analgesic
PT w/ pos UA
Why are TCAs are used in pain management and which ones are used?
Block reuptake of 5HT and NE
Amitriptyline- off label
Nortriptyline
Desipramine
Why are SSRIs/SNRIs used in pain management and which ones are used?
Block reuptake of 5HT and NE
Duloxetine- DM neuropathy, Fibromyalgia
Milnacipran- Fibromyalgia
Vanlafaxine- Neuropathic pain
Why are anti-convulsants used in pain management and which ones are used?
Decreases neuron excitability
Gabapentin- Post-Herpetic neuralgia, Neuropathic pain
Pregabalin- Diabetic neuropathy, Fibromyalgia, Post-herpatic Neuralgia
Why are local anesthetics used in pain managements and which ones are used?
Why are counter irritants used?
Lidocaine 5%: post-herpetic neualgia, Allodynia
Deplete substance P
Non-addicted opioid PTs should be tapered off by how much/how quickly?
How long of a taper do PTs taking opioids PRN need?
20-50% of original dose
None
What are reasons to change opioids?
Lack of response
Adverse effects
Change in PT status- dysphagia
Cost/personal preference
What is the gold-standard opioid?
For PTs taking long acting opioids, short acting meds should be given for break through pain and at ? dosage?
Morphine
10-15% of TDD Q1-2hrs
Define Primary HAs
Define Secondary HAs
Migraine, Tension, Cluster, Other (cough, exertion)
Head/neck trauma, Cranial/cervical vascular d/o, Infection, Psych d/o
What are the unique characteristics of migraines?
Usually unilateral Pulsating and aggravated w/ activity Nausea Photo/Phono phobia 4-72hrs
What are the unique characteristics of tension HAs?
Bilateral Pressing/Tightening that doesn't worsen w/ activity No nausea Rare photo/phonophobia Minutes-days
What are the unique characteristics of cluster HAs?
Men
Boring/Piercing that causes PT to be restless/agitated during episode
Ipsilateral Sxs
Occur frequently and last 15m-3hrs
What does the “SNOOP” acronym for finding secondary HAs stand for?
What does “POUND” acronym stand for when searching for migraines?
Systemic Neurologic Onset (sudden) Onset (late)
Pattern
Pulsatile, One-day, Unilateral, N/V, Disabling
When/why does a provider go SNOOPing for HA causes?
Acute onset of 1st/worst in life HA w/ meningitis Sxs Inc SBP +210 or DPB +120 Dec pulse/tender temporal artery Pain worse w/ laying down
What are the Dx criteria for a migraine w/out an aura?
5 attacks
Last 4-72hrs
2 of: unilateral, pulsating, intensity, aggravated by activity causing avoidance
1 of: N/V/both, photo/phono phobia
What are the Dx criteria for a migraine w/ an aura?
2 attacks
One aura Sxs: visual, sensory, speech, motor, brain stem, retinal
Two of: one aura Sx spreads over 5min or two Sxs occur in succession; Aura Sxs last 5-60min; Each aura Sx lasts 5-60min; One Sx is unilateral, Aur followed by HA in 60min
More than 50% of migraines are genetically caused by ?
Familial hemiplegic migraines- mutations in CACNL1A4 genes on Chromosome 19
Why is 5HT an important mediator of migraines?
Stimulation- triptans
Antagonizers- methysergides
Prevent uptake/release- CCBs
Inhibit serotogenic raphae neurons- Valproate
Pain from migraines originates from ?
Trigeminovascular system- regulated by serotonin neurons; activation causes release of vasoactive neuropeptides CGRP, Substance P and Neurokinan A that cause vasodilation and dural plasma extravasation which leads to inflammation
What are the 4 Phases of Migraine HAs?
1 Premonitory Sxs- hrs to day before onset, most commonly neurologic Sxs, psychosocial, autonmic or constitutional Sxs
2 Aura- Pos or Neg (most common) sensory or motor Sxs that precede the HA by 60min
3 HA- usually early morning or upon waking, most w/ nausea
4 Resolution- fatigue, mood, tender scalp and impaired concentration
How are migraine HAs cared for across attacks?
HA 1-3: Tx w/ NSAID
Unresponsive Tx in 2 or more HAs= 4th HA Tx w/ triptan
Caution for Serotonin Syndrome
How are migraine HAs cared for during attacks?
How is migraine care stratified?
HA Tx w/ NSAID, no response in 2hrs= Tx w/ triptan
HA Dx MIDAS Grade 2= Tx w/ NSAID
HA Dx MIDAS Grade 3-4= Tx w/ triptan
When treating migraines across, within or stratified across attacks, how is “successful response” defined?
Pain reduced from 3-4 down to 0-1
What are the Non-Specific, Specific and Miscellaneous acute migraine agents?
Non-Specific: analgesics, NSAIDs
Specific: Ergotamines, Triptains
Misc.: Butorphanol nasal spray, Anti-emetic (metoclopramide)
What may be a useful FIRST choice drug for acute migraines in PTs w/ mild-mod attacks or can’t take NSAIDs or ASA?
Acetaminophen, consider w/ caffeine
Inferior pain free response to other NSAIDs and ASA
What is the MOA of Butalbital in Fioricet and Fiorinal
Short acting barbiturate
APAP/Butalbital/Caffeine- not scheduled
ASA/Butalbital/Caffeine- scheduled
What is the DOC for mild/mod migraine attacks?
How long should use of this drug be limited to?
NSAIDs- Ibuprofen, Naproxen, Excedrin
Contra to NSAID: Acetaminophen (not for gastritis, ulcer, renal dz, bleeding d/o)
Less than 15 days/mon
Ergotamine must be given with ?
What are the adverse effects?
Caffeine and rectally
Constriction leading to vascular ischemia, gangrene, tonic-clonic convulsion and mania/hallucinations
What are the administration considerations for Ergotamine?
Pre-treat w/ antiemetic and start at first sign of attack
Rectal better tolerated than PO but less effective than triptans
When is the use of Dihydroergotamine a reasonable choice for HA management?
Mod-severe HA and NSAID trial/non-opioid analgesic fails
IV w/ anti-emetic for PTs w/ severe migraines
Overall preferable over Ergotamine
What 3 Triptans have the highest likelihood of consitent success?
Which two are slower and have lower efficacy?
Major side effect?
Riza, Ele, Almo (Ele has best short term/sustained benefit)
Nara, Frova
Serotonin Synd.
What are the advantages of Sumatriptan and Zolmitriptan?
When is nasal spray form more useful?
Number of dosing formulas
Faster onset and more useful for PTs w/ vomiting
9 days or less/mon
What is unique about the first dose of a Triptan?
Done in clinic w/ EKG w/ VS on PTs that are suspected to have CAD (HTN, hypercholesterol, obese, diabetic, smoker)
What is the clinical triad of Serotonin Syndrome?
Cognitive, Neuromuscular/Autonomic dysfunction
D/c offender
Benzos- anxiety/seizure
Cooling blankets for hyperthermia
Cyproheptadine- 1st gen anti-histamine
Name the 7 applicable Triptans and related comments
Almo- Sulfa group, dec dose w/ 3A4 inhibs, desmethyl metabolite
Ele- not metabolized by MAO, don’t use w/in 72hrs 3A4 inhibitors
Frova- not metabolized by MAO
Nara- not metabolized by MAO
Riza- dec dose by 5mg if PT is taking Propanolol
Suma
Zolmi- desmethyl metabolite w 2/3 potency of parent form
What anti-emetics are used during migraines?
Metoclopramide- most efficacious for N/V from migraine; significant EPS s/e
Anti-Psychotics- dopamine/serotonin antagonists (Chlorpromazine, Prochlorperazine)
5HT3 Antagonists- not efficacious, high adverse HA (Ondansetron, Granisetron)
What are the most, intermediate and least efficacious meds for migraine treatment?
Most- Aspirin, Excedrin, Ibuprofen, Triptan
Intermediate- Acetaminophen, Naproxen, Midrin, Butorphanol, Ergotamine, DHE + anti-emetic
Least- Fioricet/Fiorinal
Medication Overuse HA are AKA ?
How are they best avoided?
Analgesic Rebound HA from daily analgesic/triptans that cause 5HT down regulation
Limit migraine therapies to 2 days/wk
What are the criteria for migraine prophylaxis?
How long does it take to assess efficacy?
+4 HA/mon or duration >12hrs
1-2mon
What are the first line migraine prophylactics for pattern, heart, depression/insomnia or seizure/MD PTs?
Predictable- NSAID at time of HA
HTN/Angina/Anxiety- BB (Verapamil if BB contraindicated)
Depressed/Insomnia- TCA
Seizure/Manic Depressive- anticonvulsant
Which anti-convulsants can be used for migraine prophylaxis?
Divalproex- N/V, Asthenia, Weight gain, Hair loss, Tremor, Liver Dz, Preg Cat D, less GI than Valproate
Valproate- kidney stones, N/V, Asthenia, Weight gain, Hair loss, Tremor, Liver Dz, Preg Cat D
Topiramate- Kidney stones, Parasthesia, Weight loss, Metabolic acidosis, Sedation, Altered taste, Cleft lip/palate
What Triptans are used for migraine prophylaxis?
Frova, Zolmi, Nara
Contraindicated in PTs w/ ischemic heart dz, uncontrolled HTN, CV dz
Naratriptan is best used for ? types of migraines?
Short term prevention from menstrual associated migraine
Which BBs are used for migraine prophylaxis?
Propan, Tim, Aten, Meto
Fatigue, Tired, Dizzy, Impotence, No for Asthma PTs, Raynauds, caution w/ diabetic, may worsen depression
T/A/M- not first line BBs but may be sued w/ other therapies for PTs w/ anxiety, HTN or angina.
What CCBs are used for migraine prophylaxis?
Which NSAID can be used?
Verapamil
S/e= constipation, HOTN, bradycardia, worsening CHF
may not be seen for 8wks
Naproxen- Prevent predictable HAs
When is Botox A considered for migraines?
Why is Mg considered for phrophylaxis?
PTs w/ +15 HA days/mon or lasting +4hrs
Pregnancy
What is the most common type of primary HA?
Tension- pain originates from myofascical factors and peripheral sensitization of nociceptors
What are the pharmaceuticals of choice for tension HAs?
DOC- Acetaminophen, NSAIDs
Limit use to 9 days or less/mon
Muscle relaxants
When is prophylaxis considered for tension HAs?
What med is used?
+2/wk, +3hrs, disabliing
DOC- Amitriptyline @ bedtime
Adverse- Anti-Ach, Weight gain, OHOTN, Arrhythmias
What is the suspected cause of cluster HAs?
Hypothalamic dysfunction- altered circadian rhythms
Lab reports of abnormal melatonin, GH, testosterone and prolactin
What type of HA is the most severe of the primary HAs?
How is their presentation different than migraine PTs?
Cluster- occur at night, spring/fall w/ ipsilateral Sxs
PTs sit and rock or pace holding head
What is the criteria for cluster HAs?
5 attacks lasting 15-180min
Attack occurs w/ ipsilateral Sx
How are cluster HAs treated?
First line- Oxygen 100% by re-breather
Sumatriptan- SubQ/intranasal- most effective
Zolmitriptan, less effective but better tolerated
Ergotamine derivatives- DHE has quickest result and repeated use can break cycles but risks make them rarely used
What medication is used as prophylaxis for cluster HAs?
DOC- Verapamil
2nd Line- Lithium, can be used w/ Verapamil
(monitor trough, thyroid and renal)
What meds are used as transitional prophylaxis between cluster HAs?
Prednisone
Dihydroergotamine
What is the most common form of osteoporosis?
Where does it usually effect and what are the two types?
OA- leading cause of disability in older adults; Primary/Idiopathic is most common
Knee, Hip, Thumb
Localized- one or two sites
Generalized- three or more sites
Most preventable risk factor for OA is ?
When shaking hands w/ PTs that have OA in their hand, what might be felt?
Obesity
Herberden nodes
What topical NSAIDs can be used for OA?
Diclofenac Gel- only FDA approved for hand or knee
Diclofenac Na- knee OA
Topical Salicylates- modest short term Tx of OA
Capsaicin- muscle/joint pain, diabetic/post-herpatic neuralgia
What is the MOA of Topical Salicylates?
What are they used for?
Local COX 2 inhibition
Short term Tx of OA
What are the clinical uses of capsaicin topicals?
What are the adverse effects?
What are the precautions?
Muscle/joints pain or Diabetic/post-herpatic neuropathic pain but must be used 4x/day
Temporary burning
Eyes, mouth, groin
What is the MOA of Corticosteroids?
What are the adverse effects?
Suppresses leukocytes and reverses capillary permeability
Hyperglycermia, Edema, HTN, Dyspepsia, Adrenal suppresion
What is the use of Glucosamine?
Stimulates proteoglycan production which is in articular cartilage.
Hyaluronic acid is lube/shock absorber of synovial fluid
What is the use of Chondroitin sulfate?
Glucosamine and Aminosugars that add tensile strength to cartilage
Increases hyaluronic concentration and viscosity
What are the precautions of using Glucosamine and Chondroitin?
Safe/tolerated when used at dose x 2yrs
Interacts w/ warfarin
PO glucosamine causes kidney issues
Shellfish allergy
What are the adverse reactions of Glucosamine/Chondroitin?
What is one underlying perk in its MOA?
GI Sxs, Not FDA approved
No blood sugar increases
RA is primarily mediated activity by ? cell
How are the activated?
T-cells
Macrophages activated by cytotoxins (IL-1, TNF-a)
Increases inflammatory mediators (CRP, histamine, prostaglandins)
Increased chondrocytes/osteoclasts which increase cartilage/bone degredation
What lab results will be see in PTs w/ RA
What are the extra-articular involvements of RA?
+ RF, Elevated CRP and ESR
Nodules, Vasculitis, Pulmonary, Ocular, Cardiac, Felty’s Syndrome- splenomegaly and neutropenia
How is RA controlled and what is used for pain relief?
Dz control= DMARDS and Biologics
Pain- NSAIDs, analgesics, glucocorticoids
What class meds are used for the treatment of RA?
NSAIDs
Steroids
DMARDs- Methotrexate, Ankylating agents, Anti-malrials, Biologics
Duloxetine- FDA approved to treat MSK pain
What is the first med used for the immediate treatment of pain and inflammation of RA and can be used as adjunct while DMARDs accumulate?
NSAIDs- Ibuprofen, Meloxicam, Nabumetone, Naproxen
What drugs are used as “bridge” therapy while waiting for DMARD therapeutic effect?
What are the mainstay of treatment?
Corticosteroids
DMARDs- started w/in first 3mon of Sxs and can reduce mortality
What are the traditional DMARDs used?
What Biologics are used w/ DMARDs?
Methotrexate, Leflunomide, Hydroxychloroquine, Sulfasalazine
TNF-a Inhibitor
Non-TNF-a Co-Stimulation modulators
Biosimilar DMARDs
When are DMARD combos used?
Sx early Dz of Mod-High activity that is non-responsive to traditional DMARD monotherapy
What are the adverse effects of Methotrexate?
What is monitored for in both Methotrexate and Leflunomide?
GI- most common
W/ chronic use: Leukopenia, Cirrhosis, Pneumonia-Like Sxs
CBC w/ platelets, AST/ALT
What is Methotrexates reversal agent?
What is Leflunomide’s reversal agent?
Leucovorin
Cholestyramine
What are the adverse effects of Leflunomide?
What is the MOA of Hydroxychloroquine?
GI, Allopecia, Hepatic, Peripheral neuropathy
Inhibits movement of neutrophils and eosinophils
What is Hydroxychloroquine used for?
What are the adverse effects of it?
Anti-malarial, RA, Lupus
Decreased vision, required eye exam Q6mon
GI
Derm
What is the MOA of Sulfasalazine
What is it used for?
Prodrug cleaved in intestine to decrease IgA and IgM
Mild RA to decrease radiologic progression of Dz
UC
What are the adverse effects of Sulfasalazine use?
What are the interactions it can have?
GI, Rash, Photosensitivity
Dec sulfasalazine absorption which binds to Fe in gut
Displaces warfarin
What is the MOA of biologic DMARDs?
What are they used for?
Block cytokines or prevent stimulation needed to activate T-cells
PTs that don’t respond to first line agents (meth) or combo agents
All biologic DMARDs increase risk of ?
What is their black box warning?
Infection
Anti-TNF-a can cause increased lympho-proliferative/CAs in kids and adults
What are the predisposing factors of gout?
Loop/Thiazide diuretics
Salicylates- no ASA, use NSAIDs
Calcineurin Inhibitors- Cyclosporine/Tacrolimus- impairs renal excretion
Chemo Drugs- Hydroxyures- rapid cell lysis
Niacin
XOIs
What meds are used for acute gout flared?
What meds are used for urate lowering therapy/chronic suppression
NSAIDS, Colchicine, Glucocorticoids
XOIs, Uricosuric Agents, Uricase
When is Celecoxib an option for gout treatment?
What meds are used for PTs w/ severe pain, polyarticular attack, or gout in multiple large joints?
PTs w/ contraindications (GI) and/or intolerant to typical NSAIDs
Colchicine and NSAID
Colchicine and Oral Corticosteroid
Intra-articular steroids
What is the first line meds for acute gouty attacks in the first 24hrs
What 3 meds have FDA approval for treating acute gout attacks?
NSAID and Colchicine (only used in first 36hrs of onset)
Naproxen, Indomethacin, Sulindac
Indo/Nap- DOC for flares
What is the MOA of Colchicine?
What is it use for?
Binds to tubulin and inhibits neutrophils associated w/ gout Sxs
Treat flares
Prophylaxis for flares
What are the adverse effects of Colchicine?
Renal/Hepatic failure
Drug interactions
N/V/D
Bone marrow suppression- suppresses fast growing cells in <1% of PTs
What are the three classes of drugs used for chronic gout suppression?
XOIs- Allopurinol, Febuxostat
Uricosuric agents- Probenecid, Lesinurad
Uricase/Urate Oxidase- Pegloticase
What are the indications for giving ULTs?
What is the first line used?
Tophi on exam/imaging
Two or more acute gouty attacks/year
CDK Stage 2 or worse
Hx of Urolithiasis
XOI- Allopurinol, Febuxostat
Alternaitves if at least one XOI is contraindicated, ineffective or intolerable: Probenacid, Pegloticase
What is the MOA of Allopurinol/Febuxostat
Fout flares can occur after initiating meds, what meds are used upon initiation?
Inhibits uric acid synthesis by inhibiting xanthin oxidase which is converts xanthine into uric acid
NSAIDs or Colchicine
What are common adverse effects of XOIs?
What are the pros/cons of Febuxostst?
Rash, Leukopenia, Thrombocytopenia, Diarrhea, CV event, Drug fever
40mg= 300mg of Allo
Higher dose had better tolerance and more success
More expensive/no generic
Higher risk of thrombo emoblic events
What are the MOA of Probenecid/Lesinurad
Weak organic acids that inhibit tubule urate anion exchanger that control urate absorption
Reduced B-lactam Abs and reduces excretion of other meds
What are the clinical uses of Uricosuric Agents?
What are the adverse effects?
Probenecid- taken BID as an alternative/additive to ULT Tx if XOIs aren’t enough, contrainidcated, intolerable
Lesinurad- must only be used daily in combo w/ XOIs
Acute gouty attack- prophylact w/ NSAIDs or Colchicine
GI intolerance
Uric acid stone formation
What are the contraindications and interactions of Uricosuric Agents?
Don’t give to PTs w/ uric acid crystals in UA
PTs must hydrate
Interact w/ renally cleared meds
Reduced/rendered useless by Salicylates (no change in uric acid levels when used w/ Aspirin)
What is the MOA of Pegloticase?
What is it used for?
Recombinant Urate Oxidase that catalyzes oxidation of uric acid into allantoin
Severe gout Dz refractory to traditional urate lowering therapies
What are the adverse effects of Pegloticase?
What PTs are contraindicated from receiving it?
Flares for first 3mon
Infusion reactions
HF exacerbation
G6PD deficiency
What are the first line options of pharmacologic prophylaxis for gout?
How long should prophylaxis last?
Cochicine, NSAIDs, PPI
Alternative: oral corticosteroids
6mon
3mon after target serum levels are reached and no tophi are present w/ serum monitoring Q2-5wks
PTs return to medical and serum urate goals have not been met, what are the next steps?
Titrate single XOI to max dose
Add Uricosuric to XOI: Probenecid, Losartan, Fenofibrate (Losartan and Fenofibrate are off-label but recommended 2nd line)
If still not reached, add Pegliticase (only in severe Dz and PT is refractory/intolerant to other ULT)
What is intrinsic factor’s use in the stomach?
What stimulates HCl production?
Located in parietal cells of gastric glands and aids in absorption of B12
PPump at parietal cell by Ach, Histamine or Gastrin
What makes up the protective substances for the GI?
What is their role?
Prostaglandins E1, E2 and I2 (prostacyclin)
Inhibit basal/stimulated gastric acid secretion
On the stomach picture, what meds are linked to H Pylori, M1, ATPase, H2 and PG?
H Pylori- Bismuth, ABX M1- M antagonist ATPase- Omerprazole H2- H2 antagonist PG- misoprosotol
All GERD PT treatment starts with what steps?
Diet, Lifestyle
Mild- 1 or less episode/wk= H2 inhibitor and antacid.
After 4wks, if Sxs aren’t controlled, switch to PPI
GERD that’s >1/wk- start w/ PPI
If Sxs return, restart therapy
What are the non-invasive tests for H Pylori?
What are the invasive tests?
F Ag test
Urea breath test
Serologic
Endoscopy w/ biopsy
How are H pylori ulcers treated?
PPI
Triple therapy- Clarithromycin Amoxicillin (alt- metronidazole if allergic to PCN)
Quad therapy- PTs that can’t take Clarithromycin; Tetracycline, Metronidazole, Bismuth Subsalicylate
How long is H pylori ulcer treatment conducted for?
What follow on test must be done on all PTs?
14 days of ABX
If PUD remains, continue PPI x 4-8wks (duodenal) or 8-12wks (gastric)
Erradication testing- UBT or stool Ag
Must be off PPIx x 2wks prior
What is in Sequential Therapy after H Pylori triple therapy?
Clarithromycin, PPI, Tinidazole/Metronidazole x 10 days
Effective erradication of H Pylori in treatment naive PTs
What is the next step for PTs that are H Pylori treatment failures?
Culture
Rescue therapy- Levofloxacin, Amoxicillin, and PPI x 2wks
How are NSAID induced ulcers treated?
D/c
If d/c isn’t an option- switch to APAP or non-acetylates salicylate
COX-2 inhibitor- Celecoxib (last line)
PPI or MIsoprostol
How are stress ulcers managed prophylactically?
PPI, H2RA
IV PPI is equivalent to high dose IV H2RA
IV preferred in PTs w/ feeding tubes
What is the MOA of antacids?
What are their use in clinic?
Weak bases that neutralize acids by forming Na/H2O
1st line therapy for intermittent Sxs (less than 2x/wk)
Break through therapy for PTs on PPI/H2RA therapy
What are the adverse effects of antacids?
What drugs do they interact with?
Constipation due to Al/Ca, diarrhea from Mg, accumulation of metal elements in kidneys
Chelation- avoid Fluroquinolones and TCAs
Toxicity- HIV meds (Ralte/Saquinavir)
What is the MOA of Sodium BiCarb?
When should caution be taken during use?
Reacts w/ HCl to form CO2 and NaCl
CO2 released by belching or causes bloating
Metabolic alkalosis
High Na content, caution w/ HTN/CFH
What are the benefits of using Calcium Carbonate as an antacid?
What adverse effects can happen?
Less neutralization activity
Metabolic alkalosis
Hypercalcemia
What is the MOA of Magnesium Hydroxide?
What is an adverse effect?
When is it not used?
Reacts w/ HCl to form MgCl and H2O as an antacid or laxative
Osmotic diarrhea
Renal insufficiency
What is the MOA of Aluminum Hydroxide?
What are the adverse effects?
Reacts w/ HCl to form AlCL and H2O
Constipation
Renal insufficient shouldn’t take it
What two forms of antacids are often used together to reduce the impact on bowel function?
How does Aluminum Hydroxide and Magnesium Trisilicate work?
Mg/Al Hydroxide and Simethicone
Simethicone relieves flatulence
Alfinic acid that forms foamy layer above stomach contents to reduce reflux
What is the MOA of H2RAs?
What are the adverse effects?
Competitively block histamine from binding to H2 receptors on parietal cells to inhibit gastric acid and secretion
CNS and confusion- most common
Prolonged cimetidine use- rare gynecomastia
What drugs interact with H2RAs?
Cimetidine- competes w/ meds and creatinine for tubular secretion in kidney
What are the diasdvantages of Cimetidine?
First H2 blocker
Endocrine effects- anti-androgen
Competes w/ meds and creatinine for tubular secretion in kidney
What are the characteristics of the H2RA Ranitidine
Few s/e w/ good efficacy
150mg BID
Preferred H2RA for IV use
What med is an antacid and H2 antagonist combo?
Nizatidine has comparable efficacy as other H2RAs, what is it’s con?
Famotidine
Expensive
What is the disadvantage of PPIs
What drugs fall into this class?
Most expensive agents for GERD management
-prazole
Panto, Ome, Esome, Rabe, Lanso, Dexlanso
What is the MOA of PPIs?
What is the adverse risk of taking these?
Prodrug that irreversibly bind to H/K/ATPase pump to suppress H+
Fx risk, Hypomagnesiaemia, C Diff, Community acquired pneumonia
What interactions do PPIs ahve?
FDA recommends avoiding Ome and using Pantoprazole as alternative
Drugs w/ pH dependent absorption: Ketoconazole, Itraconazole, Protease inhibitors
What are the mucosal protective agents?
What are they used for?
Sucralfate- covers/protects ulcers and stimulates prostaglandin release but reqs acid for activation
Heals ulcers, not as effective as H2 blockers/PPIs
Mainly- preventing stress related bleeding
Why is Sucralfate use limited?
What are the mucosal protective agents?
Multiple doses/day, Large tablets, needs for meal/drug seperation
Misoprostol
Bismuth Subsalicylate
What is the MOA of Misoprostol?
What are they used for?
E1 prostaglandin analog w/ antisecretory and mucosal protective properties
Preventing NSAID induced ulcers, not used widely due to adverse profile and multiple daily doses
What are the adverse effects of Misoprostol?
What are the contraindications of use?
Diarrhea, Abd pain
Pregnancy X
What are the Prokinetic Agents?
Metoclopramide
Erythromycin
What is the MOA and use of Metoclopramide
Dopamine antagonist that stimulated upper GI w/out effecting secretions while enhancing tissue effect to ACh to enhance motility and blocking 5HT receptors for anti-emetic effect
Reflux, N/V from chemo, Impaired GI emptying
What are the adverse effects of Metoclopramide?
CNS- drowsy, restless
EPS- parkinsonian features
What is the MOA and use of Erythromycin as a prokinetic
What are the adverse effects?
Stimulate GI smooth muscles and promotes onset of migrating motor complex
IV for PTs w/ gastroparesis
Cramping and bacterial resistance
Where is the vomiting center located in the brain?
What 4 sources of afferent input can stimulate it?
Medulla
Solitary Tract Nucleus- dopamine/5HT3 receptors
Vestibular apparatus- H1 /muscarinic cholinergic receptors
Chemo Trigger Zone- 5HT3, D2 H1 and M1, Opioid receptors
Cerebral cortex- sight, smell, emotions
What causes vomiting undigested food hours after eating?
What causes vomiting immediately after meals?
What causes vomiting in mornings after breakfast?
Gastroparesis, Gastric outlet obstruction
Bulimia, Psychogenic causes
Pregnancy, Uremia, Alcohol, Increased ICP
What anti-emetics are used for general medical use?
Which ones are used for chemo induced vomiting?
Phenothiazines, Serotonin antagonists
Phenothiazines, Serotonin antagonists, NK1 antagonists, Dronabinol
What anti-emetics are used for post-op vomiting?
Which ones are used for motion sickness?
Serotonin antagonists, Scopolamine
Antihistamines, Scopolamine
Which anti-emetics are used for pregnancy induced vomiting?
Which one is used for gastroparesis?
Phosphorylated Carbohydrates, Pyridoxine, Antihistamines
Metocopramide
What are the 5HT3 Antagonists?
What is given with them?
Ondansetron, Granisetron, Dolasetron,
Palonosetron
Corticosteroids- Dexamethasone, Methylprednisolone
What is the MOA of 5HT3 antagonists?
What are they used for?
Block presynaptic serotonin receptors on vagal fibers and vomit center and CTZ
Post-op N/V (Ondansetron)
Chemo N/V w/ Corticosteroids
Radiation N/V
What are the most common s/e from 5HT3 antagonist use?
HA, Dizzy, Constipation
Small QTc prolongation especially w/ Dolasetron use
What is the MOA of anti-histamines?
What are the 1st Generation Antihistamine?
Block vestibular apparatus H1s preventing N/V from motion sickness, all have drowsiness and anti-Chl s/e
Pregnancy Cat-A
Meclizine, Diphenhydramine, Dimenhydrinate, Doxylamine/Pyridoxine (B6)
What is the MOA of Phenothiazines?
What two drugs are included?
Block D/M/H receptors in CTZ for anti-emetic effect given PO, IV, IM, rectal (not SubQ)
Prochlorperazine- N/V
Promethazine-N/V/Motion Sick
What are the adverse effects of Phenothiazines?
HOTN, Restlessness, EPS, Drowsy
What is unique about Promethazine’s administration route?
What class of drug is it?
No Sub-Q, IV needs to be diluted to prevent tissue necrosis
1st generation Antihistamine
What is the MOA and use for Scopolamine?
Cholinergic antagonist w/ more lipophilic/central effects
Motion sickness
Surgery adjunct- blocks short term memory formation
Blocks salivation
What needs to be monitored in PTs taking Scopolamine?
What are the adverse effects?
HR, Temp, Urine output
Excessive Anti-Chl effects
What is the MOA of Butyrophenones?
What are they used for?
Droperidol
Blocks dopamine receptors in CTZ of CNS
No longer used as antipsychotic
Post-Op N/V
Endoscopy/surgery sedation in combo w/ opiod/benzos
What are Adverse Effects of using Butyrophenones?
EPS, Dystonia, Drowsy, Aggitation, Confusion
What Benzamide is used and what is it’s MOA and use?
Metoclopramide
Trimethobenzamide
Blocks emetic impulse to CTZ w/out EPSx like Metoclopramide
Apomorphine pre-treatment of Parkinson’s
Post-op N/V
Gastroenteritis nausea
When are cotricosteroids used for N/V?
What two are used?
Chemo induced N/V w/ 5HT3 antagonists
Dexamethasone
Methylprednisolone
When are Benzos used for N/V?
What two are used?
Prior to chemo to reduce anticipatory N/V caused by anxiety
Lorazepam
Diazepam
What two Cannabinoids are used for N/V and what are the info facts on them?
Dronabinol- synthetic, Unresponsive Chemo nausea AIDS anorexia Potentiates psychoactive agents Store @ 46-59*F
Nabilone- C-2
Synthetic, nausea from chemo that’s refractory to other anti-emetics
What are the NK1s used for N/V
Aprepitant
Fosaprepitant
Netupitant/Palonosetron
Facts of Aprepitant
Blocks postrema in medulla
Modulates Sub. P
Augments 5HT3 receptor
Used w/ 5HT3 antagonists and steroids for acute/delayed Cisplatin-induced emesis
Facts of Fosaprepitant
Prodrug, converted to Aprepitant 30m after infusion
Used for Mod-High emetogenic chemo
Facts of Netupitant/Palonosetron
Netupitant- antagonist of Substance P and NK1 receptors
Palonsetron- 5HT3 antagonist
All NK1s used for N/V have what similar adverse characteristic?
Multiple CYP3A4 interactions
What are the 4 types of diarrhea?
Secretory- large volume w/ E+
Altered motility- ANS s/o (DM, Post-Vagotomy, Hyperthyroid, IBS, Addisons)
Osmotic- hyperosmolar gradient in intestine from carb malabsorption, lactase deficiency, fat malabsorption, short bowel syndrome
Inflammatory- IBD, C Diff, E Coli, Shigella, Neoplasm
Criteria for mild, moderate and severe diarrhea
How are mild and moderate treated?
3 or less, 4 or more, 6 or more
Mild- hydrate, lactose free diet, avoid caffeine
Mod- anti-motility, rehydrate
What ABX are used for Traveler’s diarrhea?
Fluoroquinolones
Azithromycin
Rifaximin- only owrks in colon
What ABX treats IBS diarrhea dominant disease?
Rifaximin
What drugs are used for treating ABX associated diarrhea (C Diff)?
Metronidazole, PO Vancomycin
What is the MOA and Use of Loperamide
Mu opioid agonist/Meperidine derivative, inhibits Ach and decreases peristalsis w/out crossing BBB
MIld-Mod non-invasive diarrhea Sxs
First line choice anti-diarrheal for acute diarrhea
Less sedating/addicting than Diphenoxylate
What are the adverse and contras for Loperamide?
PTs w/ severe colitis
When is Diphenoxylate w/ Atropine used for diarrhea?
What are the adverse effects and times it shouldn’t be used?
Mod-Severe non-invasive diarrhea
Refractory diarrhea
Suboptimal to Loperamide or Bismuth
No analgesia
Higher/longer use can cause dependence
Not for children
PTs w/ severe colitis
What miscellaneous agents are used for diarrhea?
Bismuth Subsalicylate- Traveler’s Diarr.
Octerotide- inhibs GH, Tx tumor/HIV associated diarrhea
Lactase enzyme- lactase deficiency/intoelrance
Probiotics- bacteria overgrowth in sm. int., C Diff treatment
What is the MOA of Osmotic Laxatives
What is it used for?
Moves water into distal small bowel/colon causing high volume liquid stool
Acute/intermittent constipation
Pre-op/procedure prep
What are the adverse effects of osmotic laxatives?
Na Phosphate- may cause hypoE+, hypernatremia, nephropathy
MgSulfate- caution w/ renal impairment, will cause Mg intoxication, E+ abnormalities
What is the MOA of non-absorbable osmotic laxatives?
What is it used for?
Metabolized by bacteria to increase osmotic pressure, causing increased fluids/cramps
Acute, intermittent, chronic constipation
When is Lactulose use preferred?
Chronic liver dz
Prevention of hepatic/portal encephalopathy
Reduce ammonia levels
When is Polyethylene glycol solution used?
Endoscopic/radiology pre-op prep
Ingested 2-4L over 2-4hrs
Safe for Liver Dz and Pregnancy
When is PEG 3350 powder use for constipation preferred?
Chronic constipation
IBS constipation w/ less cramping/gas
Safe for Liver/Renal Dz and Pregnancy
When is Glycerin Suppository use preferred for constipation?
When is Mineral Oils used?
Acute to intermittent constipation in Peds Pts
Mild constipation and need for intestinal lube
Avoid aspiration
Potential for lipoid pneumonia (lipids in lungs)
What triptan for short term relief of menstrual related migraines
Nara
Where do the following DMARDs work? Abatacept Methotrexate Lefunomide Tocilizumab Anakinra
Abatecept- stimulation of dendrite to T cell
Meth/Leflu- CD4 to B or Macrophage
Ana- IL-1
Tocil- IL-6
Where do Etanercept/ I/A/G/Cmabs work?
TNF-a
Use and adverse facts of Infliximab
Combo w/ Meth, not for monotherapy
Ankylosing spond.
Infusion reaction
Activation of latent TB
Use and adverse facts of Etanercept
Meth failures, JRA
Infection and CA risk
Facts of Non-TNF Co-Stim Adatacept, , and
Aba- used for severe RA in PTs w/ incomplete response to DMARDs or TNF-a antagonists
Binds to CD80 and CD86 to inhibits T cells
Can be used w/ Meth of non-bio DMARD
Facts of Non-TNF Co-Stim Rituximab
Combo w/ Meth
Doesn’t activate TB
Binds to CD-20
Used in leukemia, hodgkin and Plyangiitis PTs
Don’t give as bolus/push
Reaction to first infusion, give w/ corticosteroids
Heb B reactivation
Facts of Non-TNF Co-Stim Rituximab
Combo w/ Meth
Doesn’t activate TB
Binds to CD-20
Used in leukemia, hodkin and Plyangiitis PTs
Facts of Non-TNF Co-Stim Tocilzumab
For PTs not responded to TNF-a
IL-6 antagonist
Facts of Non-TNF Co-Stim Tofacitnib
JAK inhibitor
Adverse effects of Abatecept
HA, URI
Hypersensitivity
What triptans can be administered ODT, MLT, SubQ and Intransal?
Riza- sublingual
Suma- SubQ, Nasal
Zolmi- sublingual, Nasal
Alma- sulfa allergy
Acronym for Tension HA management
Acronym for Cluster HA management
T: AcNRA
C: OSZEVL/PD
Acronym for Tension HA management
Acronym for Cluster HA management
T: AcNRA
C: OSZEVL/PD
What is the treatment for RA
NSAID- Meloxicam, Ibuprofen, Nabumetone, Naproxen Steroid- Prednison DMARD- M L S H Biologics- T N B (ICAGE) Duloxetine- FDA Tx for MSK pain
Sequence for gout treatment
Flare- N C G
ULT- XOI (AF), UA (Pro, Lesi), Uricase (Peglo, Rasbur)
H Pylori ulcer treatment
PPI, Clarithromycin, Amoxicillin (Triple Therapy) (substitute amoxicilin w/ metron if PT penicillin allergic)
Retreatment/no clarithromycin/areas of high clarithromycin resistance= Tetracycline, Metronidazole, Bismuth Salicylate (Quad therapy)
NSAID ulcer treatment
Reduce/switch to APAP or non-acetylated salicylate
Celecoxib- last line
PPI or Misoprostol
Stress ulcer treatment
Recommended for ICU PTs
PPI and H2RA
IV PPI equivalent to IV H2RA
PT w/ feeding tube gets enteric formulation of either
Rifaxamin usage and facts
MOA: alters bacterial content in GI
Use: IBS-D for global Sx relief; E Coli induced traveler’s diarrhea in PTs w/ Hepatic
Encephalopathy
Adverse: Nausea, ALT increase, C Diff eval if no improvement
Caution: liver impairment
Eluxadoline MOA, Use, Adverse and C/C
MOA: Mu/K agonist, D antagonist that lessen bowel contractions in IBS-D
Use: Adults w/ IBS-D
Adverse: Spincter of Odi spasms, Pancreatitis
Contra: Bile obstruction, Pancreatitis, +3 drinks/day
5HT3 Antagonist MOA, Use, Adverse and Warning
MOA: affect visceral pain, increase motility and GI secretions
Use: women w/ IBS-D
Adverse: only avail through Prometheus Rx program
Warning: Ischemic Colitis, Constipation
5HT3 Antagonist
MOA: affect visceral pain, increase motility and GI secretions
Use: women w/ IBS-D
Adverse: only avail through Prometheus Rx program
Warning: Ischemic Colitis, Constipation
IBS-C female older than 18=
IBS-C in women=
IBS-C=
IBS-D in women:=
Lubiprostone
Tegaserod
Linaclotide
Alosetron
Drugs for IBS-C
Laxative
Cl activator: Lubiprostone
5ht4 agonist: Tegaserod
Drugs for IBS Pain/Bloating
Antispasmodic: Dicyclomine, Hyoscyamine
MOA: block Ach in PNS
Use: adjunct to IBS med for PRN pain relief
Drugs for IBS Pain/Bloating
Antispasmodic: Dicyclomine, Hyoscyamine
MOA: block Ach in PNS
Use: adjunct to IBS med for PRN pain relief
TCAs for IBS-C
SSRIs for IBS-D and IBS-C:
Amitriptyline, Nortriptyline, Imipramine
Fluoxetine, Setraline, Citalopram, Paroxetine
What medications are used as adjuncts for IBD/o
Loperamide- proctitis, diarrhea
Anti-Achl- Dicyclomine, Hyoscyamine
Aminosalicylates for IBD/o
First line for IBD
Anti-inflammatory w/ little systemic absorption
Sulfasalazine metabolized to active mesalamine
Crohns and UC
Mesalamine- fewer allergic reactions
Aminosalicylates for IBD/o
First line for IBD
Anti-inflammatory w/ little systemic absorption
Sulfasalazine metabolized to active mesalamine
Crohns and UC
Mesalamine- fewer allergic reactions
Naloxegol OIC
Substrate for PEG and Naloxone derivative
Adult PTs w/ OIC w/ chronic non-CA pain
Naloxegol OIC
Substrate for PGlycoprotein transport
Adult PTs w/ OIC w/ chronic non-CA pain
Guanylate cyclase C Agonist
Lincaclotide
induces Cl and BiCarb secretion and decrease visceral pain
IBS-C; CIC
Diarrhea
Contraindicated for <17, dehydration risk
Cl Channel Activators
Activates CIC-2 to stimulate Cl secreation
Female >18y/o w/ IBS-C, CIC, OIC w/ non-CA
R/o pregnancy prior
N/Diarrhea/Dyspnea
Cl Channel Activators
Activates CIC-2 to stimulate Cl secreation
Female >18y/o w/ IBS-C, CIC, OIC w/ non-CA R/o pregnancy prior
N/Diarrhea/Dyspnea
Stimulant Laxatives
Misacodyl
Acts on nerves of colon
Constipation, pre-op prep in conjunctino w/ PEG solution
Castor Oil
Reduced to ricinoleic acid to stimulate peristalsis
Don’t use in pregnancy
Senna
Causes water/E+ secretion
Combo w/ Docusate for Constipation/OIC
Cramping, E+ disturbance
What is a gluten free bulk laxative?
Which one can be used w/ Celiac Dz?
Wheat Dextrin
Synthetic fiber Methylcellulose`
What can be used for antacid AND for laxative?
Magnesium Hydroxide
What can be used for antacid AND for laxative?
Magnesium Hydroxide
Contraindications for giving triptans?
Hx ischemic heart dz (angina, previous MI)
Uncontrolled HTN
CV dz (stroke)
Hemiplegic/Basilar migraine
How many aura for PTs to Dx w/ migraine?
2 auras= Dx w/ migraine
What is contained in Bismuth
Metronidazole
Tetracycline
Use of Octerotide
HIV diarrhea
Tumor diarrhea
Use of Octerotide
HIV diarrhea
Tumor diarrhea
What are the adverse effects of using Cimetidine
Gynecomastia
Inhibits CYP 450
Competes w/ meds and creatinine for secretion
Dont give to PTs on several drugs
What are the adverse effects of using Cimetidine
Gynecomastia
Inhibits CYP 450
Competes w/ meds and creatinine for secretion
Dont give to PTs on several drugs
When to start Senna
Don’t give PT Meperidine if they’ve taken ? drug?
Long term prevention of OIC by causing water and E+ to secrete into bowel
MAOI
When to start Senna
Long term prevention of OIC by causing water and E+ to secrete into bowel
How quickly are pharmacologic initiated for initial gout treatment?
Within 24hrs
Use of Lubiprostone
Stims Cl secretions into intestine for IBS-C females +18y/o
CIC
OIC w/ non CA pain
How long should PTs that have been on long term opioids tapered off?
10%/wk or 5-20%/mon
Not addicted= 20-50%/wk
What drug is used for life saving constipation and required FDA approval for use?
When is Alosetron use preferred?
Tegaserod
Female IBS-D
What drugs can’t be taken while taking uricosuric agents?
How frequently can Naloxone be given?
Salicylates
Q2-5min
What has Ondansetron use been popular with?
What is the first line choice for anti-diarrheal for acute diarrhea
Anti-emetic for peds w/ gastroenteritis
Adult/Post-op N/V
Loperamide
Which XOI is more likely to achieve target uric acid levels when levels are <6mg/dl
What drug can be used for OIC and given SubQ?
Febuxostat
Methynaltrexone