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. 2016 Nov 16;17(1):1–28. doi: 10.1007/s40268-016-0153-9

Table 3.

Medications reported to induce xerostomia, salivary gland hypofunction, or sialorrhea with moderate level of evidence

Drug name and function ATC code Mechanism and site of action Number of citations for: Sources per level of evidence (n) Total publications (n) References
Oral ‘dryness’ Sialorrhea
Xerostomia SGH Subjective Objective A2 B2 A3 B3
Amisulpride (atypical anti-psychotic) N05AL05 Antagonist to dopamine and 5-HT 1 0 0 0 1 0 0 1 2 [157, 203 a]
Asenapine (atypical anti-psychotic) N05AH05 Antagonist to dopamine, 5-HT, histamine (H1) and α(1,2) adrenergic receptors 2 0 0 0 0 1 0 1 2 [115, 204]
Atenolol (anti-hypertensive/anti-arrhythmic) C07AB03 β1-Adrenergic antagonist 1 0 0 0 0 1 0 0 1 [205]
Azelastine (anti-allergic) R01AC03, Histamine (H1) antagonist 1 0 0 0 0 1 0 0 1 [206]
Cetirizine (anti-allergic) R06AE07 Histamine (H1) antagonist 2 0 0 0 0 1 0 1 2 [206, 207]
Clobazam (anxiolytic/anti-convulsant) N05BA09 Benzodiazepine—enhances the GABA effect on its receptors 0 0 0 1 0 1 0 0 1 [208]
Darifenacin (urological—reduces bladder activity) G04BD10 Anti-muscarinic 5 1 0 0 1 2 0 3 6 [133135, 137, 138, 171]
Desipramine (anti-depressant) N06AA01 Preferential NE-reuptake inhibitor 2 0 0 0 1 1 0 0 2 [91, 209 a]
Desloratadine (anti-allergic/anti-pruritic) R06AX27 Histamine (H1)-antagonist, anti-muscarinic 2 0 0 0 0 1 0 1 2 [210, 211]
Desvenlafaxine (anti-depressant) N06AX23 5-HT and NE reuptake inhibitor 5 0 0 0 0 3 0 2 5 [52, 212215]
Dexfenfluramine (appetite suppressant) A08AA04 Releases 5-HT 2 0 0 0 0 1 0 1 2 [216, 217]
Dexmedetomidine (hypnotic sedative) N05CM18 α2-Adrenergic agonist 1 0 0 0 0 1 0 0 1 [218]
Didanosine (anti-viral—HIV-1 therapy) J05AF02 Nucleoside analog reverse transcriptase inhibitor 1 0 0 0 0 1 0 0 1 [219]
Dihydrocodeine (opioid-analgesic) N02AA08 Weak agonist for the μ-opioid receptor 1 0 0 0 0 1 0 0 1 [220]
Dosulepin (anti-depressant) N06AA16 Non-selective 5-HT/NE reuptake inhibitor, anti-muscarinic, anti-histamine (H1) 1 0 0 0 0 1 0 0 1 [221]
Doxepin (anti-depressant) N06AA12 Non-selective 5-HT/NE reuptake inhibitor, anti-muscarinic, anti-histamine (H1), α1-adrenergic receptor antagonist 2 0 0 0 0 1 0 0 1 [92]
Ebastine (anti-allergic/anti-pruritus) R06AX22 Histamine (H1) antagonist 2 0 0 0 0 3 0 0 3 [222224]
Enalapril (anti-hypertensive) C09AA02 ACE inhibitor 2 0 1 0 0 1 0 0 1 [205]
Eszopiclone (hypnotic-sedative) N05CF04 Enhances the GABA effect on its receptors 3 0 0 0 0 1 0 2 3 [225227]
Etravirine (anti-viral—HIV-1 therapy) J05AG04 Non-nucleoside reverse transcriptase inhibitor 1 0 0 0 1 0 0 0 1 [219]
Fentanyl (opioid-analgesic) N01AH01, N02AB03 Strong µ-opioid receptor agonist 1 0 0 0 0 1 0 0 1 [218]
Fesoterodine (urological - reduces bladder activity) G04BD11 Anti-muscarinic 4 0 0 0 0 3 0 1 4 [181, 183, 228230]
Haloperidol (anti-psychotic) N05AD01 Antagonist to dopamine, 5-HT, histamine (H1), muscarinic and α(1,2)adrenergic receptors 2 0 1 0 0 2 0 0 2 [24, 119]
Hyoscyamine (anti-peristaltic/spasmolytic) A03BA03 Anti-muscarinic 1 0 0 0 0 1 0 0 1 [231]
Isradipine (anti-hypertensive) C08CA03 Calcium channel blocker—arterial vasodilator effects 1 0 0 0 0 1 0 0 1 [205]
Lamivudine (anti-viral—HIV, hepatitis B) J05AF05 Nucleoside analog reverse transcriptase inhibitor 1 0 0 0 1 0 0 0 1 [219]
Levocetirizine (anti-allergic) R06AE09 Histamine (H1) receptor antagonist 1 0 0 0 0 1 0 0 1 [232]
Lisinopril (anti-hypertensive) C09AA03 ACE inhibitor 1 0 0 0 0 1 0 0 1 [233]
Lurasidone (anti-psychotic) N05AE05 5-HT/dopamine antagonist, α2-adrenerg receptor antagonist, partial 5-HT(7)-agonist 1 0 0 0 0 1 0 0 1 [234]
Maraviroc (anti-viral) J05AX09 Prevents HIV from entering the cells 1 0 0 0 1 0 0 0 1 [219]
Methyldopa (anti-hypertensive) C02AB01 False transmitter; synthesis of the less potent α-methyl-NE instead of NE 2 0 1 0 0 1 0 1 2 [50, 53]
Metoprolol (anti-hypertensive/anti-arrhythmic) C07AB02 β1-Adrenergic receptor antagonist 1 1 0 0 0 1 1 0 2 [14, 235]
Mexiletine (anti-arrhythmic) C01BB02 Sodium channel blocker 1 0 0 0 0 1 0 0 1 [236]
Morphine (opioid-analgesic) N02AA01 Strong agonist on the µ-receptor 2 0 0 0 0 2 0 0 2 [237, 238]
Naltrexone (treatment of alcoholism) N07BB04 Opioid receptor antagonist 1 0 0 0 0 1 0 0 1 [239]
Nevirapine (anti-viral—HIV-1) J05AG01 Non-nucleoside reverse transcriptase inhibitor 1 0 0 0 1 0 0 0 1 [219]
Nicotine (for smoking cessation) N07BA01 Agonist to nicotinic receptors 2 0 0 0 0 2 0 0 2 [240, 241]
Orlistat (anti-obesity) A08AB01 Inhibits lipase, that breaks down dietary triglycerides 1 0 0 0 0 1 0 0 1 [169]
Pregabalin (anti-convulsant by non-GABAergic mechanisms) N03AX16 Reduces transmitter release 3 0 0 0 0 1 0 2 3 [242244]
Raltegravir (anti-viral—HIV-1) J05AX08 Prevents the integration of virus DNA into host chromosomes 1 0 0 0 1 0 0 0 1 [219]
Saquinavir (anti-viral) J05AE01 HIV protease inhibitor 1 0 0 0 1 0 0 0 1 [219]
Sertindole (anti-psychotic) N05AE03 Antagonist to dopamine, 5-HT and α1-adrenergic receptors 2 0 0 0 0 1 0 1 2 [245, 246]
Sodium valproate (anti-convulsant) N03AG01 Reduces the excitability of nerves by inhibiting the inflow of sodium ions 1 0 0 0 0 1 0 0 1 [114]
Tapentadol (opioid-analgesic) N02AX06 Weak µ-opioid antagonist, and neuronal NE-reuptake inhibitor 1 0 0 0 0 1 0 0 1 [247]
Terazosin (urological—decreases urinary flow obstruction/anti- hypertensive) G04CA03 α1-Adrenergic receptor antagonist 1 0 0 0 0 1 0 0 1 [248]
Tizanidine (anti-muscle-spasticity) M03BX02 Releases GABA from spinal cord inhibitory interneurons, in addition weak α2-adrenergic agonist 2 0 0 0 2 0 0 0 2 [28, 249]
Tolvaptan (diuretic) C03XA01 Vasopressin V2 receptor antagonist preventing the action of the anti-diuretic hormone (ADH) 1 0 0 0 0 1 0 0 1 [250]
Tramadol (opioid-analgesic) N02AX02 Weak µ-opioid receptor agonist and NE/ 5-HT reuptake inhibitor 1 0 0 0 0 1 0 0 1 [237]
Trospium (urological—reduces bladder activity) G04BD09 Muscarinic receptor antagonist 4 0 0 0 0 2 0 2 4 [128, 132, 133, 137]
Zopiclone (hypnotic) N05CF01 Non-benzodiazepine—enhances the GABA effect on its receptors 1 0 0 0 0 1 0 0 1 [251]

5-HT 5-hydroxytryptamine (serotonin), ACE angiotensin-converting enzyme, ATC Anatomical Therapeutic Chemical, GABA gamma-aminobutyric acid, NE norepinephrine, SGH salivary gland hypofunction

aAnimal study