Drugs Flashcards
Nitazenes
Benzimidazole opioids, also known as nitazenes, are a class of synthetic opioids with an unusual benzimidazole structure often referred to as opioid New Psychoactive Substances (opioid NPS).
Like other synthetic opioids, benzimidazole opioids bind the mu-opioid receptor and may exhibit potency up to several hundred times that of morphine
Drospirenone
Drospirenone is a progestin and antiandrogen medication which is used in birth control pills to prevent pregnancy and in menopausal hormone therapy, among other uses.[1][8] It is available both alone under the brand name Slynd and in combination with an estrogen under the brand name Yasmin among others.
Droe-SPY-re-nown
Alone: Slynd
With estradiol: Angeliq
With ethinylestradiol: Yasmin, Yasminelle, Yaz, others
With estetrol: Nextstellis
Shingrix
Approved indication: prevention of herpes zoster and postherpetic neuralgia
If free Zostavax, wait 5 years. If paid Zostavax wait 12 months. Immunocompetent people should delay Shingrix® for at least 12 months after an episode of herpes zoster.
This new vaccine is a recombinant form of the herpes zoster glycoprotein E antigen, also known as Hz/su. It does not contain live virus and therefore may be suitable for immunocompromised patients pending the results of further studies
Vaccination involves two 0.5 mL intramuscular injections, preferably in the deltoid muscle, with a two-to-six-month interval between doses.
for participants aged 70 years and older, the vaccine efficacy was 91.3%
The vaccine may be given at the same time as seasonal influenza vaccine, but at a different site.
Tolvaptan
Approved indication: hyponatraemia
Samsca (Aspen)
15 mg and 30 mg tablets
A new approach is to target the action of antidiuretic hormone (vasopressin). Tolvaptan is an antagonist at the vasopressin V2 receptor. By blocking the binding of antidiuretic hormone to the receptor, tolvaptan increases the excretion of water. As there is no significant change in sodium excretion, the serum concentration of sodium increases.
The serum sodium begins to rise 2–4 hours after an oral dose, with a peak effect at 4–8 hours. Treatment is given once a day, starting at 15 mg. The dose can be increased, but the effect on serum sodium does not increase beyond 60 mg daily.
Finerenone
Approved indication: chronic kidney disease associated with type 2 diabetes with albuminuria
Kerendia (Bayer)
10 mg and 20 mg film-coated tablets
Steroidal mineralocorticoid-receptor antagonists (MRAs), such as spironolactone, may preserve kidney function, but are associated with increased risk of hyperkalaemia.2,3 Finerenone is a novel nonsteroidal MRA that is associated with a lower risk of hyperkalaemia than steroidal MRAs.
Finerenone’s approved indication is to delay progressive decline of kidney function in adults with chronic kidney disease (with albuminuria) associated with type 2 diabetes who are already taking the maximum tolerated dose of an angiotensin converting enzyme inhibitor (ACEI) or angiotensin II receptor blocker (ARB).
Low Dose Naltrexone
LDN may improve symptoms in patients with FM by changing the processes of central and peripheral sensitisation.15 LDN in the range 1–5 mg/day operates beyond its typical role of opioid receptor antagonist and exerts immunomodulatory and anti-inflammatory effects through glial cells in the CNS and peripheral nervous system.15,18 LDN is thought to antagonise Toll-like receptor 4 activity in glial cells and consequently reduce activation of the inflammatory cascade and nociceptive system.15,18 An in vitro biochemical study on microglial cells has provided evidence that naltrexone is a neuroprotective substance that could be a promising novel treatment for various neuroinflammatory conditions.19 Another proposed analgesic mechanism is reactive upregulation of endogenous opioid production due to transient and partial opioid receptor blockade.20
Tirzepatide
Once weekly Mounjaro
Tirzepatide is a long-acting dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Both receptors are present on the pancreatic α and β endocrine cells, brain, heart, vasculature, immune cells (leukocytes), gut and kidney. GIP receptors are also present on adipocytes.
Tirzepatide is selective to human GIP and GLP-1 receptors. Tirzepatide has high affinity to both the GIP and GLP-1 receptors. The activity of tirzepatide on the GIP receptor is similar to native GIP hormone.
Type 2 Diabetes Mellitus:
Mounjaro is indicated for the treatment of adults with insufficiently controlled type 2 diabetes mellitus as an adjunct to diet and exercise
as monotherapy when metformin is not tolerated or contraindicated.
in addition to other medicinal products for the treatment of type 2 diabetes.
The starting dose of tirzepatide is 2.5 mg once weekly. After 4 weeks, increase the dose to 5 mg once weekly.
If needed, dose increases can be made in 2.5 mg increments after a minimum of 4 weeks on the current dose. The recommended doses are 5 mg, 10 mg and 15 mg. The 2.5 mg, 7.5 mg and 12.5 mg are not maintenance doses.
The maximum dose of tirzepatide is 15 mg once weekly.
Guanfacine hydrochloride
Approved indication: attention deficit hyperactivity disorder
Intuniv (Shire) 1 mg, 2 mg, 3 mg and 4 mg modified-release tablets If drug treatment is necessary, psychostimulants such as dexamfetamine and methylphenidate are considered. Atomoxetine is another option and sometimes clonidine is used. Like clonidine, guanfacine hydrochloride is an agonist of the alpha2 adrenergic receptor. Its effects in ADHD are uncertain, but guanfacine does not stimulate the central nervous system.
The new product is a modified-release formulation with peak plasma concentrations reached five hours after the dose is taken. It has a half-life of 18 hours and is suitable for once-daily dosing (morning or evening). The target dose is guided by the child’s weight
Like clonidine, guanfacine can lower blood pressure. Hypotension and bradycardia are common adverse effects.
Regular measurement of height and weight is recommended during treatment. However, the body mass index of most patients will remain in the same category while taking guanfacine.6
Guanfacine is therefore reserved for children and adolescents 6–17 years old who cannot take or who have had an inadequate response to stimulants or atomoxetine.
Brexpiprazole
Approved indication: schizophrenia: Rexulti
0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets
Brexpiprazole is a new antipsychotic for schizophrenia. It is structurally similar to aripiprazole and has a similar mechanism of action. It acts at many receptors. For example, it is a partial agonist at serotonin 5-HT1A and dopamine D2 and D3 receptors and an antagonist at the serotonin 5-HT2A and noradrenergic receptors. Brexpiprazole can be taken with or without food. The starting dose is 1 mg. This should be titrated to the recommended target dose of 2–4 mg over eight days depending on clinical response and tolerability.
The 4 mg/day dose of brexpiprazole seems to be effective for acute schizophrenia in short-term trials. Up to half of the patients responded to this dose.1,2 In a longer term placebo-controlled trial, brexpiprazole reduced the risk of relapse in patients already established on brexpiprazole.4 As with other antipsychotics, akathisia and weight gain are common. Brexpiprazole has been approved as an adjunct treatment of major depression in the USA but not in Australia.
Atomoxetine
- Atomoxetine (Strattera) is a noradrenaline reuptake inhibitor used for treating children, adolescents and adults with attention deficit hyperactivity disorder (ADHD). Methylphenidate and dexamphetamine remain first-line drug treatments for ADHD. Atomoxetine is subsidised on the Pharmaceutical Benefits Scheme for people who cannot take psychostimulants.
- Treatment should be based on a comprehensive diagnosis and employ behavioural, psychosocial and educational strategies according to individual needs. Atomoxetine is not a psychostimulant and appears to have a low potential for abuse and diversion. It does not require State or Territory department of health permission to prescribe.
- Atomoxetine shares some adverse effects with psychostimulants, including loss of appetite and increased blood pressure, but may cause less sleeplessness. The long-term safety profile of atomoxetine is unknown.
- Atomoxetine may increase the risk of suicidal thoughts and behaviours. Monitor children taking atomoxetine for warning signs.
- Be aware of potential cardiovascular adverse effects; people with symptomatic cardiovascular disease should not use atomoxetine.
Actikeral 0.5%/10% solution
Combining low-potency 0.5% fluorouracil cream with 10% salicylic acid> (Actikerall™) has also been shown to be effective for actinic keratoses on the face and hands and forearms over a 12-week course. It is especially useful for hyperkeratotic (horny) lesions.
The primary outcome of Study 0702 was the proportion of patients with complete clearance of a single pre-defined target AK lesion eight weeks after end of treatment, and 5-FU/SA was statistically significantly superior to placebo for this end point.
Arexvy
RSV pre F3.
Vaccine for prevention of RSV in older adults.
An adjuvanted recombinant RSV vaccine. Single dose of 0.5ml by intramuscular injection. for adults greater than or equal to 60 years of age.
ATAGI recomendations:
All adults aged 75 or over
ATSI 60-74
Adults 60-74 with medical conditions which increase risk of RSV.
Can be co administered with Flu, covid, prevenar and Shingrix.
Do not administer to pregnant women or infants.
Nirsevimab
Brand name Beyfortus. Injectable long acting Monoclonal antibody (mAb) that protects against RSV for a least 5 months after a single dose.
Qld: All infants born from 1-2-24. Offered at time of birth or prior to discharge from hospital. Infants not immunised in hospital can access Nirsevimab up to less than 8 months of age.
Young children with certain complex medical conditions from 8 months to 20 months until 31-10-24.
ABRYSVO
RSVpreF (Abrysvo) vaccine is the ONLY Respiratory Syncytial Virus (RSV) vaccine approved for use during pregnancy to protect infants from RSV-associated lower respiratory tract infection (LRTI). The vaccine should be administered during weeks 32 through 36 of pregnancy (i.e., 32 weeks 0 days through 36 weeks 6 days).
Individuals 60 years of age and older ABRYSVO is administered as a single dose (0.5 mL).
Inclisiran
Leqvio
The recommended dose of Leqvio is 284 mg administered as a single subcutaneous injection: initially, again at 3 months, followed by every 6 months.
Leqvio is indicated as an adjunct to diet and exercise to reduce low-density lipoprotein cholesterol (LDL-C) in adults with heterozygous familial hypercholesterolaemia, atherosclerotic cardiovascular disease, or at high risk of a cardiovascular event:
in combination with a statin or statin with other lipid‐lowering therapies in patients unable to reach LDL‐C goals with the maximum tolerated dose of a statin or,
alone or in combination with other lipid‐lowering therapies in patients who are statin-intolerant
Inclisiran is a cholesterol-lowering double-stranded small interfering ribonucleic acid (siRNA), conjugated on the sense strand with triantennary N-acetylgalactosamine (GalNAc) to facilitate uptake by hepatocytes. In hepatocytes, inclisiran utilises the RNA interference mechanism and directs catalytic breakdown of messenger RNA (mRNA) for proprotein convertase subtilisin/kexin type 9. This increases low density lipoprotein cholesterol (LDL-C) receptor recycling and expression on the hepatocyte cell surface, which increases LDL-C uptake and lowers LDL-C levels in the circulation.
