Pharmacology II
🫁 Respiratory System 🔒
→ 📷
- intermittent
- mild Persistent
- moderate persistent
- severe persist.
- status asthmaticus
- short acting b2 agonist (salbutamol/albuterol)
- systemic steroids (methyl-prednisone oral or hydrocortisone i.v.)
- anticholinergics (iptratropium bromide)
- Methylxanthines
+Epinephrine
→ 📷
- Inhaled steroids (fluticasone/budesoide)
- Long acting b2 agonist (salmeterol/formoterol)
- Leukotriene Modifier (Montekast; Zileuton)
- Theophylline
- Systemic steroids
MABs (Omalizumab) (+ Chromes)
Allergen specific immunotherapy
H1 antagonists
spirometry:
Post-bronchodilator FEV/FVC < 0.7
assessment of airlow limitation
Grade | FEV (% predicted) |
GOLD 1 | ≥80 |
GOLD 2 | 50-79 |
GOLD 3 | 30-49 |
GOLD 4 | <30 |
SABA + SAMA
steroids
(theophylline i.v.)
(AB if purulent sputum)
T
↑cAMP (via adenylyl cyclase stimulation) → ↓Ca release 📷 → SM relaxation
FFFF → thats why steroids are needed
↓R activity (downregulation) + tachyphylaxis
inhaled
- severe persistent asthma
- children
- short (4-6h)
- long, (8-12h)
- ultralong (12-24h)
exacerbation of asthma + COPD
Controllertherapy
in asthma (+ICS)
COPD ( mono or with LAMA/ICS → see above)
(exception: Formoterol combination can be given in exacerbation)
COPD
usually not → but sometimes if high doses or systemic administration!
- Heart -tachycardia -palpitation, -arrhythmias
- Skeletal muscles -tremor -muscles cramps
- CNS -headache -anxiety
salbutamol
2 puffs PRN, 3-5min interval; Ømore than 8 puffs/day
Terbutaline
Dont disTERB me while sniffing The BUTtER-LINE
status asthmaticus
(when refractory to classic treatment - salbutamol)
Fenoterol (another SABA)
(1) Salmeterol
(2) Formoterol
(Salute ∝ Salmeterol)
(Formation ∝ Formoterol)
controllertherapy in asthma + copd
(+/- together with ICS)
formoterol + ICS (budesonide/beclomethasone)
→ can be given in exacerbation + controller therapy of asthma
Formoterol can also be with SAMA in COPD or bronchitis w/ spasm
COPD
Antimuscarinic (LAMA) or steroids (ICS)
- Indacaterol
- Olodaterol
- Vilanterol
- Carmoterol
"Carmo + Krooked sagen Ola zum Villain Inder-Kater"
(Carmo + kooked = ultrageil = ultralong)
block m1 + m3 📷 → bronchodilation + ↓mucous secretion (via vagus)
- COPD #1 exacerbation (SAMA) + controller ( LAMA (+SAMA in A))
- Severe asthma attacks (SAMA)
- Persistent asthma (+b2)
short: ipratropium bromide
long: tiotropim bromide
↑hyperreactivity after treatment stop
(+antimuscuarinic symptoms)
early + late
(1)Non-selective PDE inhibitor
(2) Adenosine receptor antagonist
(3) Histone deacetylases activitation
(∴ ↑ cAMP)
⇒ Bronchodilation
⇒ + anti-inflammatory effect:
inhibits NF-kB translocation, increases IL-10 release, Anti-oxidative, Induces apoptosis of neutrophils and eosinophils)
- CNS stimulation
- Diuretic effect * → ↓Preload
- ↑HR
☕
oral + IV!
iv → asthma + COPD reliever
oral → asthma + (COPD controller)
MAINLY RELIEVER THERAPY never 1st line
(CAVE: narrow therapeutic index! → more of a last resort)
genetic + environmental factors → means inter-personal variability (→ not really predictable)
(1) CNS effects incl. tremor (+agitation, insomnia, seizures)
(2) Tachycardia + Arrhythmias
→ like to much coffee
hypotension (↓preload + ↑HR→ ↓output)+ seizure (refractory; due to ↑CNS)
chest pain + death (heart affected)
>20
seizures (more prone than acute tox)
prophylactic diazepam (2nd line: barbiturate)
- Epilepsy
- Acute MI + IHD
- Hypertension
- Cave: elderly + newborns
- tea/coffee consumption
Amino-phylline
(1) ↓ Inflammation (2) ↓ Leukocyte infiltration (Importantly, they also upregulate (2 receptors)
T (alone or in combination)
severe + freq. exacerbation (Stage D)
- oral + iv → asthma exacerbation
- iv → status asthmatic, patient is vomiting
- Systemic → COPD exacerbation
- oral → controller in chronic severe asthma (step 5)
oral → methylprednisolone + prednisone
iv → hydrocortisone, methylprednisolone sodium succinate
T
T
- oral candidiasis
- dysphonia
- ↓bone density
- Fluticasonide
- Budesonide
- Flunisolide
- Controller - asthma
- alternative for ICS in NSAID induced asthma
- asthma + allergic rhinitis
LTBA (IL-8 also potent neutrophil chemoattractant. IL-8 looks like IL-B)
LTC4, D4, E4 (Also ↑ Airway vascular permeability and mucus production)
CysLT1. (= Leukotriene receptor)
receptor for LT-D4, -C4, -E4. 📷
Montelukast + Zafirlukast
- Systemic Eosinophilia
- Vasculitis (Churg-strauss)
- Neuro-psychiatric symptoms
esp. in children
nightmares, sleep disturbance, mood disorders, aggressive behavior
Monte ist verrückt rot und reitet auf nem strauss
Zileuton
↓LT A4,B4 + C4,D4,E4
(sie läuten an den Dino-Eiern)
↑Liver enzymes (hepatotox)
Aspirin (NSAIDs in general)
inhibition of COX shifts the AA metabolism to the LOX leukotriene pathway (exaggerated in aspirin-induced asthma)
Mild-moderate asthma persistent
On Mast cells:
↓Histamine release by mastcells
💪 stabilizing mast cells ( ↓ mast cell “degranulation”)
↓bronchial hyperreactivity in (long term)
F → early + later
T
Methylxanthines
inhaled
- lungs: cough + bronchospasm
- more above: laryngeal edema + bitter taste
- headache + nausea
Farbe zu Inhalieren schadet Rachen, Lungen und Kopf
Omalizumab
→ bindings prevents mast cell sensitization (IgE cant bind to mastcells → no degranualation)
moderate - severe persist. asthma (controller)
s.c. (every 2-4weks)
F → well tolerated
children <6y
(Nimm keine Süßigkeiten von Omas an)
Benralizumab
Mepolizumab, Reslizumab
Severe eosinophilic asthma
sc or iv.
administer allergens → progressive dose inc.
(for houst dust mites)
asthma PLUS allergic rhinitis
sedation
Cetirizine, Loratadine
- 👃🏼 Drugs for Allergic rhinitis
- 💦 Anti-Coughs and Mucolytics
🫀 Cardiovascular System 🔒
- 💠 ACE Inhibitors
- 🛑 ARBs
- 🎰 Direct renin inhibitors
- 🍦 Calcium channel blockers
- 🎺 Beta Blockers
- Basics
- 🌊 Diuretics
- 💠 ACEi, ARBs + Aliskiren
- 🎺 Beta blockers
- 🍦 Calcium channel blockers
- #2 Line Drugs
- 🤰🏽 HT in pregnancy
- 👴🏼 HT in elderly
- 🚑 Hypertensive Emergency
- Basics
- 🧨 Nitrates
- 🎺 Beta blockers
- 🍦 Calcium channel blockers
- Other #2nd line drugs that can be used in anti-anginal treatment?
- Combined therapy
- Drug-eluting endovascular stents
- 🦵🏼 Treatment of PAD
- Basics
- Class I - 🥜 Na-Channel-Blockers
- Class II - 🎺 Beta-Blockers
- Class III - 🍌 K-Channel-Blockers
- Class IV - 🍦 Ca-Channel-Blockers
- Other antiarrhythmics
- ❤️🩹 Drugs in Heart Failure
🧠 Nervous System 🔒
- Basics
- 🥞 Benzodiazepines
- 💤 Non-benzodiazepine hypnotics aka Novel BZD-R agonists aka Z-compounds
- ✂️ Barbiturates
- Other sedative-hypnotics
- Basics
- 🛵 TCAs (TriCyclic antidepressants) - First generation antidepressants
- 🙂 SSRIs (Selective serotonin re-uptake inhibitors)
- SNRI (Serotonine and noradrenalin re-uptake inhibitors)*
- Serotonine receptor antagonist (5-HT2 receptor antagonists / NASSA)*
- NDRIs (Noradrenalin and dopamine re-uptake inhibitors)*
- NRIs (NorAdrenalin re-uptake inhibitors)
- Atypical antipsychotics
- Basics
- 1️⃣ FGA - Typical (first generation) Neuroleptics
- 2️⃣ SGA - Atypical (second generation) Neuroleptics
- Drugs for Mania
- 👵🏼 Drugs for Parkinson Disease
- ⚡ Anti-epileptics
- 💪🏼 Muscle relaxants
- 💉 Drugs Abuse and Dependence